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搜索结果：“jwh 250”

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GSK2982772

Catalog No. A19380
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RIP1 kinase inhibitor

GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively. 了解更多

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CBL-0137

Catalog No. A16836
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p53 activator / NF-κB 抑制剂

CBL0137 (CBL-0137)在基于细胞的p53和NF-kB报告基因检测中分别激活p53和抑制NF-kB，EC50为0.37 uM和0.47 uM。它还抑制组蛋白伴侣FACT（促进染色质转录复合物）。了解更多

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PK11007

Catalog No. A16833
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p53 activator

PK11007是一种抗p53药物，可通过两个表面暴露的半胱氨酸的选择性烷基化来稳定野生型和突变型p53，而不会损害其DNA结合活性。它不仅通过重新激活p53发挥抗肿瘤功能，还通过其他细胞机制发挥作用，例如将细胞ROS升高至毒性水平并激活UPR。了解更多

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Apogossypolone (ApoG2)

Catalog No. A16314
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Bcl-2 抑制剂

Apogossypolone (ApoG2)是一种Bcl-2的非肽小分子抑制剂。了解更多

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Apoptosis Inhibitor (M50054)

Catalog No. A13058
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Apoptosis 抑制剂

Apoptosis Inhibitor (M50054)是细胞可渗透的凋亡诱导抑制剂。了解更多

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p53 and MDM2 proteins-interaction-inhibitor chiral

Catalog No. A15201
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p53-MDM2 interaction 抑制剂

p53和MDM2蛋白相互作用抑制剂手性是p53和MDM2蛋白之间相互作用的抑制剂。了解更多

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Episilvestrol

Catalog No. A15080
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Apoptosis inducer

Episilvestrol是Silvestrol的衍生物，它可以通过线粒体/凋亡途径在LNCaP细胞中诱导凋亡，而不会激活执行子caspase-3或-7。5'myc-UTR-LUC抑制剂（IC50 = 0.8 nM）。了解更多

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Bcl-2 Inhibitor

Catalog No. A13580
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Bcl-2 抑制剂

Bcl-2 Inhibitor包含两种互变异构体的混合物。一种有效的，细胞可渗透的Bcl-2抑制剂与Bak BH3肽竞争体外结合Bcl-2和Bcl-XL的作用（分别为IC50 = 10 uM和7 uM）。了解更多

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- 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
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Idasanutlin (RG7388)

Catalog No. A14211
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MDM2/p53 抑制剂

Idasanutlin (RG7388)是一种有效的选择性p53-MDM2抑制剂。了解更多

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GSK2656157

Catalog No. A13577
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PERK 抑制剂

GSK2656157是PERK酶活性的ATP竞争性抑制剂，IC50为0.9 nmol/L。对于PER（K）IC50值> 100 nmol/L，对300种激酶组合具有高度选择性。了解更多

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- Cao W, .et al. Hoxa5 alleviates obesity‐induced chronic inflammation by reducing ER stress and promoting M2 macrophage polarization in mouse adipose tissue, J Cell Mol Med, 2019, Aug 23 PMID: 31441588
- Kosuke Ishikawa, .et al. A highly sensitive trap vector system for isolating reporter cells and identification of responsive genes, Biology Methods and Protocols, 2018, 1–10
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MDM2 Inhibitor

Catalog No. A13582
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MDM2 抑制剂

MDM2 Inhibitor是一种细胞可渗透的硼烷基查尔酮，表现出与MDM2的强结合，并不可逆地破坏MDM2/p53蛋白复合物。了解更多

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PRIMA-1

Catalog No. A13581
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p53 reactivator

PRIMA-1是一种小分子，因其p53再激活作用而被鉴定。了解更多

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ABT-199 (Venetoclax)

Catalog No. A12500
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Bcl-2 抑制剂

ABT-199 (Venetoclax) 是一种所谓的BH3类似药物，旨在阻断Bcl 2蛋白的功能。了解更多

Product Citations (6)

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- 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
- Anna L Koessinger, .et al. Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics, Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. Apoptotic stress-induced FGF signalling promotes non-cell autonomous resistance to cell death, Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Martin Grundy, .et al. Predicting effective pro-apoptotic anti-leukaemic drug combinations using co-operative dynamic BH3 profiling, PLoS One, 2018, 13(1): e0190682 PMID: 29298347
- Joanne Dai, .et al. Intracellular BH3 profiling reveals shifts in anti-apoptotic dependency in B-cell maturation and activation, J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
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GSK2606414

Catalog No. A12792
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PERK 抑制剂

GSK2606414是口服有效的选择性PERK抑制剂，IC50为0.4 nM。了解更多

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- Linhao Xu, .et al. Suppression of CHOP Reduces Neuronal Apoptosis and Rescues Cognitive Impairment Induced by Intermittent Hypoxia by Inhibiting Bax and Bak Activation, Neural Plasticity, 2021, 23 Aug
- Takashi Shimizu, .et al. PERK inhibition attenuates vascular remodeling in pulmonary arterial hypertension caused by BMPR2 mutation, Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333
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QNZ (EVP4593)

Catalog No. A12748
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NF-κB 抑制剂

QNZ抑制转录因子NF-κB的激活，已被用于研究NF-κB信号传导。了解更多

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Sabutoclax

Catalog No. A12823
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Bcl-2 抑制剂

Sabutoclax (BI-97C1)是pan-Bcl-2抑制剂，包括Bcl-xL，Bcl-2，Mcl-1和Bfl-1，IC50分别为0.31 μM，0.32 μM，0.20 μM和0.62 μM。了解更多

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- Christopher D. Graham, .et al. BH3 mimetics suppress CXCL12 expression in human malignant peripheral nerve sheath tumor cells, Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968
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Tenovin-1

Catalog No. A11943
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p53 activator

Tenovin-1是p53转录活性的小分子激活剂，可防止MDM2介导的p53降解。了解更多

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PAC-1

Catalog No. A11090
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Caspase activator

PAC-1是procaspase-3的激活剂，可诱导癌细胞凋亡，EC50为2.08μM。了解更多

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- 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
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TW-37

Catalog No. A10955
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Bcl-2 抑制剂

TW-37是Bcl-2的小分子抑制剂，可抑制胰腺癌细胞的生长，并通过一种涉及Notch-1和Jagged-1失活的新途径介导的胰腺癌细胞凋亡。了解更多

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VX-765 (Belnacasan)

Catalog No. A10984
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Caspase-1/4 抑制剂

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。了解更多

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- Arjun Thapa, .et al. Danger-associated molecular pattern molecules take unexpectedly a central stage in Nlrp3 inflammasome-caspase-1-mediated trafficking of hematopoietic stem/progenitor cells, Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity, Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging, Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer's disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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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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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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PETCM

Catalog No. A15308
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Caspase-3 activator

PETCM是caspase-3的激活剂，也是HeLa细胞质中凋亡小体形成的刺激物。了解更多

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Acetate gossypol

Catalog No. A14795
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Bcl-2 抑制剂

Acetate gossypol是一种从棉籽中分离出来的多酚化合物，可通过模仿BH3来抑制Bcl-2。了解更多

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Lenalidomide (CC-5013)

Catalog No. A10522
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Ubiquitin ligase inducer

Lenalidomide (CC-5013)是Thalidomide的衍生物。在体外，Lenalidomide具有三种主要活性:直接抗肿瘤作用、抑制肿瘤细胞的微环境支持和免疫调节作用。它通过抑制骨髓基质细胞支持、抗血管生成和抗破骨细胞生成作用以及免疫调节活性直接和间接诱导肿瘤细胞凋亡。了解更多

Product Citations (4)

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- Daniel A. Rauch, .et al. Interferon regulatory factor 4 as a therapeutic target in adult T-cell leukemia lymphoma, Retrovirology, 2020, 17: 27 PMID: 32859220
- 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
- Kumar R, .et al. Novel combination of tanshinone I and lenalidomide induces chemo-sensitivity in myeloma cells by modulating telomerase activity and expression of shelterin complex and its associated molecules, Mol Biol Rep, 2018, Oct 11 PMID: 30311125
- 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

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