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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

Product Citations (9)

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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
- 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
- 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
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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(R)-Bicalutamide

Catalog No. A10008
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Androgen Receptor 拮抗剂

(R)-Bicalutamide是一种活性的竞争性非甾体雄激素受体拮抗剂，对MDA 453细胞的IC50为0.17μM。了解更多

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Axitinib

Catalog No. A10103
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VEGFR 抑制剂

Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。了解更多

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- Youcef M. Rustum, .et al. Non-Coding Micro RNAs and Hypoxia-Inducible Factors Are Selenium Targets for Development of a Mechanism-Based Combination Strategy in Clear-Cell Renal Cell Carcinoma-Bench-to-Bedside Therapy, Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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SRT1720 HCl

Catalog No. A10862
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SIRT1 Activator

SRT1720 HCl是一种抑制剂，旨在作为瑟土因亚型SIRT1的小分子活化剂。了解更多

Product Citations (7)

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- Eleni Pitsillou, .et al. Interaction of small molecules with the SARS-CoV-2 main protease in silico and in vitro validation of potential lead compounds using an enzyme-linked immunosorbent assay, Comput Biol Chem, 2020, 89: 107408 PMID: 33137690
- Jie Ren, .et al. Melatonin prevents chronic intermittent hypoxia-induced injury by inducing sirtuin 1-mediated autophagy in steatotic liver of mice, Sleep Breath, 2018, Nov 8 PMID: 30411173
- Rowlands BD, .et al. Acetate metabolism does not reflect astrocytic activity, contributes directly to GABA synthesis, and is increased by silent information regulator 1 activation, J Neurochem, 2017, Mar;140(6):903-918 PMID: 27925207
- Adam Khader, .et al. SRT1720, a sirtuin 1 activator, attenuates organ injury and inflammation in sepsis, J Surg Res, 2017, Nov;219:288-295 PMID: 29078895
- Adam Khader, .et al. Sirtuin 1 Stimulation Attenuates Ischemic Liver Injury and Enhances Mitochondrial Recovery and Autophagy, Crit Care Med, 2016, Aug; 44(8): e651-e663 PMID: 26963320
- Benjamin D. Rowlands, .et al. Silent information regulator 1 modulator resveratrol increases brain lactate production and inhibits mitochondrial metabolism, whereas SRT1720 increases oxidative metabolism., J Neurosci Res., 2015, Jul;93(7):1147-56 PMID: 25677687
- Khader A, .et al. Sirtuin 1 activation stimulates mitochondrial biogenesis and attenuates renal injury after ischemia-reperfusion., Transplantation, 2014, 98(2):148-56 PMID: 24918615
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XL184 free base (Cabozantinib)

Catalog No. A10996
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VEGFR 抑制剂

XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶（特别是MET和VEGFR2）的小分子。了解更多

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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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CHIR-99021

Catalog No. A10199
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GSK-3 抑制剂

CHIR99021是一种GSK-3α和GSK-3β抑制剂，IC50值分别为10和6.7 nM。了解更多

Product Citations (6)

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- Adam Pietrobon, .et al. Renal organoid modeling of tuberous sclerosis complex reveals lesion features arise from diverse developmental processes, Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Takayuki Miyoshi, .et al. Successful induction of human chemically induced liver progenitors with small molecules from damaged liver, J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Tomoki Kamatani, .et al. Evaluation of immunosuppression protocols for MHC-matched allogeneic iPS cell-based transplantation using a mouse skin transplantation model, Inflamm Regen, 2022, Feb 2;42(1):4 PMID: 35105370
- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Otsuka R, .et al. Efficient generation of thymic epithelium from induced pluripotent stem cells that prolongs allograft survival, Sci Rep, 2020, Jan 14;10(1):224 PMID: 31937817
- Yu Huang, .et al. Development of Bifunctional Three-Dimensional Cysts from Chemically Induced Liver Progenitors, Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
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AZD6482

Catalog No. A10112
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PI3K 抑制剂

AZD6482是一种PI3Kβ抑制剂，(IC50 = 0.021M)。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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Streptozotocin (Zanosar)

Catalog No. A10868
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O-GlcNAcase 抑制剂

Streptozotocin (Streptozocin,Zanosar,STZ)用于医学研究中，用于产生1型糖尿病的动物模型，该模型直接抑制NCOAT酶在体外的O-GlcNAcase活性。了解更多

Product Citations (8)

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- Andressa Braga, .et al. Free interstitial levels of metformin in the liver of healthy and diabetic Wistar rats, Braz J Pharm Sci, 2022, 58: e19674
- Yuanyuan Du, .et al. Human pluripotent stem-cell-derived islets ameliorate diabetes in non-human primates, Nat Med, 2022, Feb;28(2):272-282 PMID: 35115708
- Karemah A. Alatawi, .et al. Coconut products alleviate hyperglycaemic, hyperlipidimic and nephropathy indices in streptozotocin-induced diabetic wistar rats, Saudi Journal of Biological Sciences, 2021, 25 June
- D.H. Mhya, .et al. Evaluation of Anti-hyperglycemic Effect of Sub-fractions Derived from Ethanol-aqueous Fraction of Balanites aegyptiaca Leaves in Streptozotocin-induced Diabetic Rats, Asian J Exp Biol Sci, 2019, 12 (2): 164-172
- Stanley I. R. Okoduwa, .et al. Validation of the antidiabetic effects of Vernonia amygdalina delile leaf fractions in fortified diet-fed streptozotocin-treated rat model of type-2 diabetes, J Diabetol, 2017, 8(3): 74-85
- Stanley I. R. Okoduwa, .et al. Anti-Diabetic Potential of Ocimum gratissimum Leaf Fractions in Fortified Diet-Fed Streptozotocin Treated Rat Model of Type-2 Diabetes, Medicines (Basel), 2017, Dec; 4(4): 73 PMID: 29019956
- Stanley I. R. Okoduwa, .et al. Appropriate Insulin Level in Selecting Fortified Diet-Fed, Streptozotocin-Treated Rat Model of Type 2 Diabetes for Anti-Diabetic Studies, PLoS One, 2017, 12(1): e0170971 PMID: 28129400
- Stanley I. R. Okoduwa, .et al. Evaluation of extraction protocols for anti-diabetic phytochemical substances from medicinal plants, World J Diabetes, 2016, Dec 15; 7(20): 605-614 PMID: 28031778
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Dovitinib (TKI-258)

Catalog No. A11411
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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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

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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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LY2157299

Catalog No. A11017
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TGF-βR 抑制剂

LY2157299是一种口服活性转化生长因子β受体（TGF-βR）激酶抑制剂。了解更多

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- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
- Oguri G, .et al. Effects of methylglyoxal on human cardiac fibroblast: roles of transient receptor potential ankyrin 1 (TRPA1) channels., Am J Physiol Heart Circ Physiol., 2014, 307(9):H1339-52 PMID: 25172898
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PD184352 (CI-1040)

Catalog No. A10212
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MEK1/2 抑制剂

PD184352 (CI-1040)是一种ATP非竞争性MEK1/2抑制剂，在基于细胞的测定中，IC50为17 nM，对MEK1/2的选择性是对MEK5的100倍。了解更多

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- Sachio Suzuki, .et al. A chemogenetic platform for controlling plasma membrane signaling and synthetic signal oscillation, Cell Chem Biol, 2022, Sep 15;29(9):1446-1464 PMID: 35835118
- Masaru Yoshikawa, .et al. Synthetic Protein Condensates That Inducibly Recruit and Release Protein Activity in Living Cells, J Am Chem Soc, 2021, May 5;143(17):6434-6446 PMID: 33890764
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Bortezomib (Velcade)

Catalog No. A10160
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Proteasome 抑制剂

Bortezomib (Velcade)是26S蛋白酶体的高度选择性，可逆抑制剂。了解更多

Product Citations (13)

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- Yoshitaka Sato, .et al. Epstein-Barr virus tegument protein BGLF2 in exosomes released from virus-producing cells facilitates de novo infection, Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Shin-Ichi Makino, .et al. Impairment of Proteasome Function in Podocytes Leads to CKD, J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. Targeting Adaptive IRE1α Signaling and PLK2 in Multiple Myeloma: Possible Anti-Tumor Mechanisms of KIRA8 and Nilotinib, Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis, Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells, Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. S-like phase CDKs stabilize the Epstein-Barr virus BDLF4 protein to temporally control late gene transcription, J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. Variable Responses of MYC Translocation Positive Lymphoma Cell Lines To Different Combinations of Novel Agents: Impact of BCL2 Family Protein Expression, Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- 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
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. Tunable and reversible drug control of protein production via a self-excising degron, Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. Severe hypoxia induces complete antifolate resistance in carcinoma cells due to cell cycle arrest, Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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Cilostazol

Catalog No. A10217
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PDE3 抑制剂

Cilostazol是3型磷酸二酯酶（PDE3）的选择性抑制剂，IC50为0.2 μM，其治疗重点是cAMP。了解更多

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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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U0126-EtOH

Catalog No. A10957
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MEK 抑制剂

U0126-EtOH是MEK1和MEK2的抑制剂，IC50分别为72 nM和58 nM。了解更多

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- Hanna Galganska, .et al. Carbon dioxide inhibits COVID-19-type proinflammatory responses through extracellular signal-regulated kinases 1 and 2, novel carbon dioxide sensors, Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- 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
- Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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17-AAG (KOS953)

Catalog No. A10010
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HSP90 抑制剂

17-AAG (KOS953)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。了解更多

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- Yool Lee, .et al. Time-of-day specificity of anticancer drugs may be mediated by circadian regulation of the cell cycle, Sci Adv, 2021, 7
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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

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- 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
- 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
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CAL-101 (GS-1101, Idelalisib)

Catalog No. A10172
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PI3K 抑制剂

CAL-101 (GS-1101,Idelalisib)是PI3K的同种型选择性抑制剂，可诱导慢性淋巴细胞性白血病（CLL）细胞凋亡。了解更多

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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
- 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
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Yoshihiro Umezawa, .et al. Molecular mechanisms for enhancement of stromal cell-derived factor 1?Cinduced chemotaxis by platelet endothelial cell adhesion molecule 1 (PECAM-1), J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577
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Tianeptine sodium

Catalog No. A10931
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5-HT Receptor 激动剂

Tianeptine钠是体内和体外的选择性5-羟色胺再摄取促进剂（SSRE）。了解更多

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Butylscopolamine BR (Scopolamine butylbromide)

Catalog No. A10170
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Butylscopolamine BR (Scopolamine butylbromide)是丁基东pol碱的口服溴化物盐形式，是一种外围作用的抗毒蕈碱型抗胆碱能药。了解更多

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BMS-708163 (Avagacestat)

Catalog No. A10157
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Gamma-secretase 抑制剂

BMS-708163 (Avagacestat)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM。了解更多

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BTZ043 (BTZ038, BTZ044) Racemate

Catalog No. A10165
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DprE1 抑制剂

BTZ043 (BTZ038,BTZ044) Racemate 抑制癸二烯基磷酸基-β-d-核糖2α-表异构酶，它是一种产生致病细菌结核分枝杆菌细胞壁的酶。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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AG14361

Catalog No. A10046
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PARP 抑制剂

AG14361是一种有效的PARP抑制剂，可在MMR（错配修复）有效/不足的细胞中增强替莫唑胺（TMZ）的细胞毒性。了解更多

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- Vimal Pandey, .et al. Roscovitine effectively enhances antitumor activity of temozolomide in vitro and in vivo mediated by increased autophagy and Caspase-3 dependent apoptosis, Scientific Reports, 2019, 9, Article number: 5012
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A-966492

Catalog No. A10019
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PARP1 抑制剂

A-966492在全细胞试验中显示出对K（i）为1 nM，EC（50）为1 nM的聚（ADP-核糖）聚合酶-1（PARP-1）酶的高效力。了解更多

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Bibf1120 (Nintedanib)

Catalog No. A10137
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VEGFR 抑制剂

Bibf1120 (Nintedanib)是一种新型的三联血管激酶抑制剂，可同时抑制三种生长因子受体：VEGFR，PDGF和FGFR。了解更多

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- 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
- Chun-Jung Chang, .et al. Overcoming interferon (IFN)-γ resistance ameliorates transforming growth factor (TGF)-β-mediated lung fibroblast-to-myofibroblast transition and bleomycin-induced pulmonary fibrosis, Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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GSK1120212 (JTP-74057, Trametinib)

Catalog No. A11029
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MEK 抑制剂

GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。了解更多

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- Nao Yamagishi, .et al. Non-canonical Regulation of EGFR by the Air Pollutant 9,10-Phenanthrenequinone, Biol Pharm Bull, 2022, 45(10):1553-1558 PMID: 36184515
- Hayato Mizuta, .et al. Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer, Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Keisuke Yanagida, .et al. Sphingosine 1-Phosphate Receptor Signaling Establishes AP-1 Gradients to Allow for Retinal Endothelial Cell Specialization, Dev Cell, 2020, 52 (6), 779-793 PMID: 32059774
- 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
- Kanemaru Y, .et al. Dramatic response of BRAF V600E-mutant epithelioid glioblastoma to combination therapy with BRAF and MEK inhibitor: establishment and xenograft of a cell line to predict clinical efficacy, Acta Neuropathol Commun, 2019, Jul 25;7(1):119 PMID: 31345255
- Chul Min Park, .et al. Mechanisms for DNA-damaging agent-induced inactivation of ErbB2 and ErbB3 via the ERK and p38 signaling pathways, Oncol Lett, 2018, Feb; 15(2): 1758-1762 PMID: 29434871
- Sumi T, .et al. Trametinib downregulates survivin expression in RB1-positive KRAS-mutant lung adenocarcinoma cells, Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
- 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
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
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SGI-1776 (free base)

Catalog No. A10838
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PIM1 抑制剂

SGI-1776 (free base)是Pim1的一种新型ATP竞争性抑制剂，在无细胞试验中的IC50为7 nM，选择性是Pim2和Pim3的50倍和10倍，对Flt3和haspin也有效。阶段1。了解更多

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- Ishikawa C, .et al. Expression and significance of Pim-3 kinase in adult T-cell leukemia, Eur J Haematol, 2017, Dec;99(6):495-504 PMID: 28833639
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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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PF-04217903

Catalog No. A10711
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c-Met 抑制剂

PF-04217903是一种选择性的，ATP竞争性c-Met抑制剂，在A549细胞中IC50为4.8 nM，对致癌基因突变型敏感(对Y1230C突变型没有活性)。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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MK-1775

Catalog No. A10599
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WEE1 抑制剂

MK-1775是一种有效的体外和体内Wee1激酶抑制剂。了解更多

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 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
- 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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Aliskiren hemifumarate

Catalog No. A11123
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renin 抑制剂

Aliskiren hemifumarate是阿利吉仑的半富马酸盐形式，是批准用于治疗原发性高血压的直接肾素抑制剂，IC50为1.5 nM。了解更多

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Caffeic acid

Catalog No. A10171
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Caffeic Acid是一种羟基肉桂酸，是一种天然存在的有机化合物。了解更多

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Daptomycin

Catalog No. A10289
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DNA/RNA Synthesis 抑制剂

Daptomycin是一种脂肽抗生素，用于治疗由革兰氏阳性生物体引起的某些感染。了解更多

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- Viktoria Lazar, .et al. Antibiotic combinations reduce Staphylococcus aureus clearance, Nature, 2022, 610: 540-546 PMID: 36198788
- Shigeru Fujimura, .et al. Antimicrobial efficacy of combined clarithromycin plus daptomycin against biofilms-formed methicillin-resistant Staphylococcus aureus on titanium medical devices., J Infect Chemother., 2015, Oct;21(10):756-9 PMID: 26162777
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TAK-700 (Orteronel)

Catalog No. A11044
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CYP17A1 抑制剂

TAK-700 (Orteronel)是一种口服非甾体雄激素合成抑制剂，可选择性抑制17,20裂解酶。了解更多

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AT7519

Catalog No. A10093
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CDK 抑制剂

AT7519是多种细胞周期蛋白依赖性激酶（CDK）的抑制剂，可导致细胞周期停滞，诱导细胞凋亡和抑制肿瘤细胞增殖。作用于CDK1，2，4，6和9时，IC50为10-210 nM，对CDK3作用效果稍弱，对CDK7几乎没有抑制活性。了解更多

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Flavopiridol HCl

Catalog No. A11045
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CDK 抑制剂

Flavopiridol HCl是细胞周期蛋白依赖性激酶的抑制剂。（-）-顺式形式诱导特定肿瘤细胞的凋亡。了解更多

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LY2940680 (Taladegib)

Catalog No. A11048
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SMO 拮抗剂

LY2940680 (Taladegib)已显示可影响由Hedgehog（Hh）蛋白引发的癌细胞信号通路。了解更多

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Voriconazole (Vfend)

Catalog No. A10978
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CYP17 抑制剂

Voriconazole (Vfend)是一种三唑抗真菌剂，可以冻干粉的形式用于静脉输注溶液。了解更多

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Bafetinib (INNO-406)

Catalog No. A10119
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Bcr-Abl 抑制剂

Bafetinib (INNO-406)是一种双重Bcr-Abl/Lyn酪氨酸激酶抑制剂。了解更多

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- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- S. Dallari, .et al. Src family kinases Fyn and Lyn are constitutively activated and mediate plasmacytoid dendritic cell responses, Nat Commun, 2017, 8: 14830 PMID: 28368000
- Andrea Haerzschel, .et al. BCR and chemokine responses upon anti-IgM and anti-IgD stimulation in chronic lymphocytic leukaemia, Ann Hematol, 2016, 95(12): 1979-1988 PMID: 27542958
- Magdalena Winiarska, .et al. Inhibitors of SRC kinases impair antitumor activity of anti-CD20 monoclonal antibodies, MAbs., 2014, 6(5): 1300-1313. PMID: 25517315
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LY317615 (Enzastaurin)

Catalog No. A10356
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PKCβ 抑制剂

LY317615（Enzastaurin）是一种有效的，选择性的PKCβ抑制剂，具有抗增殖活性（IC50 =?6 nM）。了解更多

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BMS-794833

Catalog No. A10154
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c-Met 抑制剂

BMS-794833是Met和VEGFR-2的有效ATP竞争性抑制剂，IC50为1.7和15 nM。了解更多

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S3I-201 (NSC 74859)

Catalog No. A10817
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Stat3 抑制剂

S3I-201(NSC 74859)是Stat3的新型抑制剂，可在体外抑制Stat3，Stat3复合物的形成以及Stat3-DNA结合活性（IC50 = 86±33 ?M）和Stat3依赖性转录活性。了解更多

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- Bae WJ, .et al. PTPRD-inactivation-induced CXCL8 promotes angiogenesis and metastasis in gastric cancer and is inhibited. J Exp Clin Cancer Res, 2019, 38:484 PMID: 31805999
- Nishimura K, .et al. Effect of erythropoietin production induced by hypoxia on autophagy in HepG2 cells, Biochem Biophys Res Commun, 2018, Jan 1;495(1):1317-1321 PMID: 29191652
- Ethan L. Morgan, .et al. STAT3 activation by E6 is essential for the differentiation-dependent HPV18 life cycle, PLoS Pathog, 2018, Apr; 14(4): e1006975 PMID: 29630659
- Soleimani AH, .et al. Micellar nano-carriers for the delivery of STAT3 dimerization inhibitors to melanoma, Drug Deliv Transl Res, 2017, Aug;7(4):571-581 PMID: 28290050
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Candesartan (Atacand)

Catalog No. A10175
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RAAS 拮抗剂

Candesartan (Atacand)是一种血管紧张素受体阻滞剂（也称为血管紧张素II受体拮抗剂或AIIRA）。了解更多

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- Hideki Kobara, .et al. Antihypertensive drug telmisartan inhibits cell proliferation of gastrointestinal stromal tumor cells in vitro, Molecular Medicine Reports, 2020, 22(2)
- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
- Toshihide Kashihara, .et al. Angiotensin II activates CaV1.2 Ca2+ channels through β‐arrestin2 and casein kinase 2 in mouse immature cardiomyocytes, J Physiol, 2017, Jul 1; 595(13): 4207-4225 PMID: 28295363
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Abiraterone (CB-7598)

Catalog No. A10020
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CYP17 抑制剂

Abiraterone (CB-7598)是一种有效CYP17抑制剂，20裂合酶（CYP17A1）。了解更多

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Abiraterone Acetate (CB7630)

Catalog No. A11058
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CYP17 抑制剂

Abiraterone Acetate是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂。了解更多

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Vinflunine Tartrate

Catalog No. A10975
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Microtubule Associated 抑制剂

Vinflunine Tartrate是长春氟宁的酒石酸盐，它使微管不稳定，IC50为18.8 nM，并在细胞分裂过程中干扰微管的动力学。了解更多

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