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ABT-263 (Navitoclax)

Catalog No. A10022
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Bcl-2 抑制剂

ABT-263 (Navitoclax)是一种有效的Bcl-2家族抑制剂 (Bcl-2，Bcl-xL和Bcl-w的Ki <1 nmol/L)。ABT-263对Bcl- xL，Bcl-2和Bcl-w，( Ki≤1nmol/ L) 维持高亲和力，但与Mcl-1和A1的结合更弱。了解更多

Product Citations (20)

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- Rindert Missiaen, .et al. GCN2 inhibition sensitizes arginine-deprived hepatocellular carcinoma cells to senolytic treatment, Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. Characterization of radiation-induced micronuclei associated with premature senescence, and their selective removal by senolytic drug, ABT-263, Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. Predicting and affecting response to cancer therapy based on pathway-level biomarkers, Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Hiroki Akiyama, .et al. Inhibition of USP9X Downregulates JAK2-V617F and Induces Apoptosis Synergistically With BH3 Mimetics Preferentially in Ruxolitinib-Persistent JAK2-V617F-Positive Leukemic Cells, Cancers, 2020, 12 (2) PMID: 32050632
- Stephanie Ketterer, .et al. Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling, Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. Clearance of HIV infection by selective elimination of host cells capable of producing HIV, Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Anderson R, .et al. Length-independent telomere damage drives postmitotic cardiomyocyte senescence, EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259
- Shinya Ishida, .et al. Mechanisms for mTORC1 activation and synergistic induction of apoptosis by ruxolitinib and BH3 mimetics or autophagy inhibitors in JAK2-V617F-expressing leukemic cells including newly established PVTL-2, Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488
- Rhys Anderson, .et al. Length-independent telomere damage drives cardiomyocyte senescence, bioRxiv, 2018, 2018
- Ryuta Mikawa, .et al. Elimination of p19ARF?\expressing cells protects against pulmonary emphysema in mice, Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Wei TW, .et al. Aurora A and NF-κB Survival Pathway Drive Chemoresistance in Acute Myeloid Leukemia via the TRAF-Interacting Protein TIFA, Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
- Yusuke Takagi, .et al. SPIB is a novel prognostic factor in diffuse large B?\cell lymphoma that mediates apoptosis via the PI3K-AKT pathway, Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272
- Matsumoto M, .et al. Cisplatin-induced apoptosis in non-small-cell lung cancer cells is dependent on Bax- and Bak-induction pathway and synergistically activated by BH3-mimetic ABT-263 in p53 wild-type and mutant cells, Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

Product Citations (12)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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MK-2206 2HCl

Catalog No. A10003
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AKT 抑制剂

MK-2206 2HCl是Akt1/2/3的高选择性抑制剂，IC50分别为8 nM/12 nM/65 nM。了解更多

Product Citations (17)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Ali Nasrollahzadeh, .et al. Anti-proliferative activity of disulfiram through regulation of the AKT-FOXO axis: A proteomic study of molecular targets, Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. Ultradian rhythms of AKT phosphorylation and gene expression emerge in the absence of the circadian clock components Per1 and Per2, PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Rosell??-Busquets, .et al. Nystatin Regulates Axonal Extension and Regeneration by Modifying the Levels of Nitric Oxide, Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. Chronic Activation of Gp1 mGluRs Leads to Distinct Refinement of Neural Network Activity Through Non-Canonical p53 and Akt Signaling, eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. Anti-apoptotic activity of human matrix metalloproteinase-2 attenuates diabetes mellitus, Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. Profiling the surface proteome identifies actionable biology for TSC1 mutant cells beyond mTORC1 signaling, bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. The O-glycosylating enzyme GALNT2 suppresses the malignancy of gastric adenocarcinoma by reducing EGFR activities, Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. Akt activation by Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) in ovarian cancer cells, J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. Constitutive activation of p46JNK2 is indispensable for C/EBPδ induction in the initial stage of adipogenic differentiation, Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. Periostin in tumor microenvironment is associated with poor prognosis and platinum resistance in epithelial ovarian carcinoma, Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. Inhibition of IL-1R1/MyD88 signalling promotes mesenchymal stem cell-driven tissue regeneration, Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. The tumor suppressor p53 guides GluA1 homeostasis through Nedd4-2 during chronic elevation of neuronal activity., J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624
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AC220 (Quizartinib)

Catalog No. A10027
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FLT3 抑制剂

AC220 (Quizartinib)是一种有效的选择性FLT3抑制剂，对于MC4-11和A375，IC50分别为0.56±0.3 nM和> 10 mM。了解更多

Product Citations (3)

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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691. PMID: 25326874
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Hesperadin

Catalog No. A10448
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Aurora B Kinase 抑制剂

Hesperadin是一种人极光B抑制剂，IC50为40 nM，用于防止底物磷酸化。它显著降低AMPK、Lck、MKK1、MAPKAP-K1、CHK1和PHK的活性，而不抑制MKK1在体内的活性。了解更多

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- Wenbin Ji, .et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases, PLoS One, 2016, 11(4): e0153518 PMID: 27082996
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PD 0332991 HCl (Palbociclib)

Catalog No. A10701
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CDK 4/6 抑制剂

PD 0332991 HCl (Palbociclib)是一种高度选择性的CDK4/6抑制剂，它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性，具有潜在的抗肿瘤活性。了解更多

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- Hiroki Ozawa, .et al. Targeting AURKA in treatment of peritoneal tumor dissemination in gastrointestinal cancer, Transl Oncol, 2022, Feb;16:101307 PMID: 34902741
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Pirita Pekkonen, .et al. KSHV viral cyclin interferes with T-cell development and induces lymphoma through Cdk6 and Notch activation in vivo, Cell Cycle, 2014, Dec 1; 13(23): 3670-3684 PMID: 25483078
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Neratinib (HKI-272)

Catalog No. A10638
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HER2 抑制剂

Neratinib (HKI-272)是一种酪氨酸激酶抑制剂。了解更多

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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Saracatinib (AZD0530)

Catalog No. A10108
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Src/Abl 抑制剂

Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。了解更多

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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CHR2797 (Tosedostat)

Catalog No. A10208
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Aminopeptidase 抑制剂

CHR2797 (Tosedostat)是一种新型金属酶抑制剂，在体内和体外对多种肿瘤细胞系均具有抗增殖作用，并表现出选择性。了解更多

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Pomalidomide (CC-4047)

Catalog No. A10743
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TNF-alpha 抑制剂

Pomalidomide (CC-4047)是沙利度胺的衍生物，在PBMCs中IC50为13 nM，并起免疫调节剂的作用。了解更多

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Belinostat (PXD101)

Catalog No. A10122
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HDAC 抑制剂

Belinostat（PXD101）是一种HDAC抑制剂，可抑制HeLa细胞提取物中的HDAC活性，IC50为27 nM。了解更多

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- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
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Apixaban (BMS-562247-01)

Catalog No. A10082
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Factor Xa 抑制剂

Apixaban (BMS-562247-01)是一种抗凝剂，用于预防静脉血栓栓塞和静脉血栓栓塞事件。了解更多

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- Daniël Verhoef, .et al. Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors, Nat Commun, 2017, 8: 528 PMID: 28904343
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Foretinib (GSK1363089, XL880)

Catalog No. A10998
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c-MET 抑制剂

Foretinib (GSK1363089,XL880)是c-Met和VEGFR-2的多激酶抑制剂，可抑制增殖，诱导Anoikis并损害卵巢癌转移。了解更多

Product Citations (4)

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity, Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. Cabozantinib overcomes crizotinib resistance in ROS1 fusion positive cancer, Clin Cancer Res. , 2015, Jan 1; 21(1): 166–174. PMID: 25351743
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LY2784544 (Gandotinib)

Catalog No. A10546
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JAK 抑制剂

LY2784544被鉴定为对JAK2-V617F具有高度选择性，并已进入人类临床试验，用于治疗几种骨髓增生性疾病。了解更多

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Thiazovivin

Catalog No. A10928
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ROCK 抑制剂

Thiazovivin是一种Rho相关激酶（ROCK）的选择性抑制剂。了解更多

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AUY922 (Luminespib, NVP-AUY922)

Catalog No. A10659
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HSP90 抑制剂

AUY922 (Luminespib,NVP-AUY922)是一种高效的HSP90抑制剂，在Hsp90 FP结合测定中的IC50 = 21 nM，并在体外抑制多种人类癌细胞系的增殖，GI50平均为9 nM。Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。了解更多

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- Haruka Wakasa, .et al. Adverse Effects of High Temperature On Mammary Alveolar Development In Vitro, J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
- Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

Product Citations (28)

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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AZD1152-HQPA (Barasertib)

Catalog No. A10109
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Aurora Kinase B 抑制剂

AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。了解更多

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- Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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PI-103

Catalog No. A10726
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PI3K 抑制剂

PI-103是一种有效的，细胞可渗透的，ATP竞争性磷脂酰肌醇3激酶（PI3K）家族抑制剂，对DNA-PK，PI3K（p110α）和mTOR具有选择性。了解更多

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- Diane Yang, .et al. Pancreatic Differentiation of Stem Cells Reveals Pathogenesis of a Syndrome of Ketosis-Prone Diabetes, Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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TGX-221

Catalog No. A10923
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PI3K 抑制剂

TGX-221是PI3Kp110β的有效，选择性和细胞渗透性抑制剂。了解更多

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- Mostafa Khater, .et al. Gβγ translocation to the Golgi apparatus activates ARF1 to spatiotemporally regulate G protein-coupled receptor signaling to MAPK, J Biol Chem, 2021, Jan-Jun, 296:100805 PMID: 34022220
- Mostafa Khater, .et al. G protein βγ translocation to the Golgi apparatus activates MAPK via p110γ-p101 heterodimers, J Biol Chem, 2021, Jan 22;296:100325 PMID: 33493514
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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TG100-115

Catalog No. A10922
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PI3K 抑制剂

TG100-115是一种PI3Kγ/δ抑制剂（IC50值分别为83和235 nM）。了解更多

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Gefitinib (Iressa)

Catalog No. A10422
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EGFR 抑制剂

Gefitinib (Iressa)是一种EGFR抑制剂，可阻断靶细胞中表皮生长因子受体(EGFR)的信号传导。了解更多

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Mansi Srivastava, .et al. Inhibition of the TIRAP-c-Jun interaction as a therapeutic strategy for AP1-mediated inflammatory responses, Int Immunopharmacol, 2019, 71: 188-197 PMID: 30909134
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AG-1478 (Tyrphostin AG-1478)

Catalog No. A11022
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EGFR 抑制剂

AG-1478 (Tyrphostin AG-1478)是EGFR激酶的抑制剂，IC50值为3 nM。了解更多

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- Khattab M, .et al. Conformational Plasticity in Tyrosine Kinase Inhibitor-Kinase Interactions Revealed with Fluorescence Spectroscopy and Theoretical Calculations, J Phys Chem B, 2018, May 3;122(17):4667-4679 PMID: 29629773
- Muhammad Khattab, .et al. A pH-induced conformational switch in a tyrosine kinase inhibitor identified by electronic spectroscopy and quantum chemical calculations, Sci Rep, 2017, 7: 16271 PMID: 29176733
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KU-0063794

Catalog No. A10505
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mTOR 抑制剂

KU-0063794是哺乳动物雷帕霉素靶位的选择性抑制剂(分别为mTORC1和mTORC2，IC50 ~10 nM)。了解更多

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GDC-0980 (Apitolisib, RG7422)

Catalog No. A11023
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mTOR/PI3K 抑制剂

GDC-0980 (Apitolisib,RG7422)是一种有效的，I型PI3激酶和mTOR激酶抑制剂（TORC1/2），对于p110α，β，δ和γ的体外IC50为5、27、7和14 nM。了解更多

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- Kasun Wanigasooriya, .et al. Patient Derived Organoids Confirm That PI3K/AKT Signalling Is an Escape Pathway for Radioresistance and a Target for Therapy in Rectal Cancer, Front Oncol, 2022, Jul 4;12:920444 PMID: 35860583
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Acarbose

Catalog No. A10029
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Anti-Diabetic Agent

Acarbose是一种肠道alpha-glucosidase抑制剂，用于治疗2型糖尿病以及某些国家的前驱糖尿病。了解更多

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PD153035 (HCl salt)

Catalog No. A10702
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EGFR 抑制剂

PD153035 (HCl salt)是EGFR酪氨酸激酶活性的极其有效和特异的抑制剂。了解更多

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AG-014699 (Rucaparib)

Catalog No. A10045
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PARP 抑制剂

AG-014699 (Rucaparib)是一种PARP抑制剂，可抑制聚（ADP-核糖）聚合酶（PARP，后者是DNA修复中的关键酶。无细胞试验中作用于PARP1的Ki为1.4 nM，对其余8个PARP位点也有结合亲和力。了解更多

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- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
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PIK-93

Catalog No. A10731
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PI3K 抑制剂

PIK-93是第一个有效的，人工合成的PI4K(PI4KIIIβ)抑制剂，IC50为19 nM；抑制PI3Kα，IC50为39 nM。了解更多

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- Gavin Ka Yu Siu, .et al. Hepatitis C virus NS5A protein cooperates with phosphatidylinositol 4-kinase IIIα to induce mitochondrial fragmentation, Sci Rep, 2016, 6: 23464 PMID: 27010100
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BMS 599626 (AC480)

Catalog No. A11209
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EGFR 抑制剂

BMS 599626 (AC480)是一种选择性的，高效效的HER1，HER2和HER4酪氨酸激酶抑制剂（IC50分别为22、32和190 nM），具有潜在的抗肿瘤活性。了解更多

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Arry-380 analog

Catalog No. A11027
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HER2 抑制剂

Arry-380 analog是一种ErbB-2抑制剂，可选择性结合并抑制ErbB-2的磷酸化，从而导致表达ErbB-2的肿瘤细胞的生长抑制和死亡。了解更多

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AZ628

Catalog No. A11063
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Raf 抑制剂

AZ628是一种RAF抑制剂，IC50值：BRAF V600E和野生型CRAF约为30 nM，野生型BRAF约为100 nM。了解更多

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GSK690693

Catalog No. A11030
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AKT 抑制剂

GSK690693是一种新型的ATP竞争性低纳摩尔泛Akt激酶抑制剂（IC50值分别为Akt1、2和3的2、13和9 nM）。了解更多

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- Khan MI, .et al. Thalidomide attenuates development of m0rphine dependence in mice by inhibiting PI3K/Akt and nitric oxide signaling pathways, Prog Neuropsychopharmacol Biol Psychiatry, 2018, Mar 2;82:39-48 PMID: 9223784
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PHT-427

Catalog No. A11032
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AKT 抑制剂

PHT-427是一种新型的Akt/磷脂酰肌醇依赖性蛋白激酶1 pleckstrin同源域抑制剂。了解更多

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A-674563

Catalog No. A11034
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Akt 抑制剂

A-674563是一种B/Akt抑制剂，IC50为14 nM，并且还显示出对PKA和CDK2的抑制活性，IC50分别为16和46 nM。了解更多

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- Kobayashi T, .et al. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation, Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells, Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent, Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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SGX-523

Catalog No. A10839
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c-Met 抑制剂

SGX-523是一种口服生物可利用的小分子，与c-Met蛋白或HGFR特异性结合，可防止HGF结合并破坏MET信号通路。了解更多

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MGCD-265 (Glesatinib)

Catalog No. A10587
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c-Met 抑制剂

MGCD-265 (Glesatinib)是一种多靶酪氨酸激酶抑制剂，可与多种RTK（包括c-Met受体（HGFR）结合并抑制其磷酸化。Tek/Tie-2受体；VEGFR类型1、2和3；和MST1R。了解更多

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PD173074

Catalog No. A10703
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FGFR1/VEGFR2 抑制剂

PD173074是有效的，细胞可渗透的和ATP竞争性的FGFR和VEGFR抑制剂。了解更多

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- Cheryl Q.E. Lee, .et al. What Is Trophoblast? A Combination of Criteria Define Human First-Trimester Trophoblast, Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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LY2603618 (IC-83)

Catalog No. A11036
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Chk 抑制剂

LY2603618 (IC-83)是一种chk2抑制剂，可与chk2结合并抑制其活性，这可能会阻止DNA损伤剂引起的DNA修复。了解更多

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- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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SNS-032 (BMS-387032)

Catalog No. A10850
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CDK 抑制剂

SNS-032（BMS-387032）是细胞周期蛋白依赖性激酶（Cdks）2、7和9的高度选择性和有效抑制剂，具有体外生长抑制作用，并具有诱导恶性B细胞凋亡的能力。了解更多

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Danoprevir (RG7227)

Catalog No. A10284
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HCV NS3/4A protease 抑制剂

Danoprevir (RG7227)是HCV NS3/4A丝氨酸蛋白酶的有效抑制剂。了解更多

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- Mahim Khan, .et al. Hesperidin identified from Citrus extracts potently inhibits HCV genotype 3a NS3 protease, BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Inês GARCEZ PALHA, .et al. An in vivo translation-reporter system for the study of protein synthesis in zebrafish embryos, Biol Open, 2018, Nov 7 PMID: 30404898
- Hui Shen, .et al. Inhibitory Effects of Caffeic Acid Phenethyl Ester Derivatives on Replication of Hepatitis C Virus, PLoS One., 2013, 8(12): e82299 PMID: 24358168
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VX-222

Catalog No. A10980
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HCV Protease 抑制剂

VX-222是HCV NS5B聚合酶的小分子非核苷抑制剂，正在研究中，用于治疗丙型肝炎病毒感染。了解更多

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- Wataru Ito, .et al. Isolation and characterization of hepatitis C virus resistant to a novel phenanthridinone derivative, Antivir Chem Chemother, 2015, Dec; 24(5-6): 148-154 PMID: 27503576
- Hui Shen, .et al. Inhibitory Effects of Caffeic Acid Phenethyl Ester Derivatives on Replication of Hepatitis C Virus, PLoS One., 2013, 8(12): e82299 PMID: 24358168
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Bleomycin sulfate

Catalog No. A10152
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DNA/RNA Synthesis 抑制剂

Bleomycin Sulfate硫酸博来霉素是一种糖肽类抗生素，也是一种鳞状细胞癌(SCC)抗癌剂。了解更多

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- Mai Kanemaru, .et al. Nanoparticle-mediated local delivery of pioglitazone attenuates bleomycin-induced skin fibrosis, J Dermatol Sci, 2018, Jan;93(1):41-49 PMID: 30655107
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Gemcitabine HCl (Gemzar)

Catalog No. A10423
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DNA/RNA Synthesis 抑制剂

Gemcitabine HCl (Gemzar)是一种DNA synthesis抑制剂，作用于PANC1，MIAPaCa2，BxPC3和Capan2细胞，通过在癌细胞dna复制过程中取代核酸的一个组成部分，防止肿瘤生长。了解更多

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- G. R. Iglesias, .et al. Hyperthermia-Triggered Gemcitabine Release from Polymer-Coated Magnetite Nanoparticles, Polymers, 2018, 10(3), 269
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CHIR-124

Catalog No. A11046
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CHK 抑制剂

CHIR-124是一种新型有效的Chk1抑制剂（Chk1和Chk2的IC50：分别为0.32 nM和697 nM）。了解更多

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Silibinin (Silybin)

Catalog No. A10842
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Silibinin (Silybin)是Silymarin化合物的主要活性成分。了解更多

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LY2228820 (Ralimetinib)

Catalog No. A10545
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p38 MAPK 抑制剂

LY2228820 (Ralimetinib)是一种新型强效p38MAPK抑制剂，具有强效抗炎活性。了解更多

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Kaempferol

Catalog No. A10495
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ERRα and ERRγ inverse 激动剂

Kaempferol被发现抑制Ki为0.3-0.5 μM的牛主动脉肌球蛋白轻链激酶，并且还被发现通过新的ERK-NFκB-cMyc-p21途径抑制VEGF表达和体外血管生成。了解更多

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Crenolanib (CP-868596)

Catalog No. A11052
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PDGFR/FLT3 抑制剂

Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。了解更多

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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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Salbutamol sulfate (Albuterol)

Catalog No. A10819
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Adrenergic Receptor 激动剂

Salbutamol sulfate (Albuterol)是一种短效β2肾上腺素能受体激动剂。了解更多

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