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ABT-737

Catalog No. A10255
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Bcl-2 抑制剂

ABT-737是一种类BH3抑制剂，能同时抑制Bcl-xL，Bcl-2和Bcl-w，EC50分别为78.7 nM，30.3 nM和197.8 nM;但对Mcl-1，Bcl-B及Bfl-1没有抑制作用。了解更多

Product Citations (15)

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- Jung Mo Lee, .et al. ABT-737, a BH3 Mimetic, Enhances the Therapeutic Effects of Ionizing Radiation in K-ras Mutant Non-Small Cell Lung Cancer Preclinical Model, Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. Utilizing in vitro drug release assays to predict in vivo drug retention in micelles, Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. OAS1/RNase L executes RIG-I ligand-dependent tumor cell apoptosis, Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. Invariant natural killer T cells coordinate removal of senescent cells, Med, 2021, 2,1-13
- Ying Ji, .et al. Use of ratiometrically designed nanocarrier targeting CDK4/6 and autophagy pathways for effective pancreatic cancer treatment, Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. The senotherapeutic drug ABT-737 disrupts aberrant p21 expression to restore liver regeneration in adult mice, Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- 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
- Hsu CC, .et al. α7-Nicotine acetylcholine receptor mediated nicotine induced cell survival and cisplatin resistance in oral cancer, Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. Lysophosphatidic acid promotes survival of T lymphoma cells by altering apoptosis and glucose metabolism, Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- 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
- Jose Mario Gonzalez-Meljem, .et al. Stem cell senescence drives age-attenuated induction of pituitary tumours in mouse models of paediatric craniopharyngioma, Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. Sorafenib targets the mitochondrial electron transport chain complexes and ATP synthase to activate the PINK1-Parkin pathway and modulate cellular drug response, J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. ABT-737 Synergizes with Cisplatin Bypassing Aberration of Apoptotic Pathway in Non-small Cell Lung Cancer, Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. Critical contribution of MCL-1 in EMT-associated chemo-resistance in A549 non-small cell lung cancer, Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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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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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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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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HA14-1

Catalog No. A11448
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Bcl-2 抑制剂

HA14-1与Bcl-2相互作用，抑制Bcl-2的抗凋亡作用。了解更多

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Obatoclax mesylate (GX15-070)

Catalog No. A10665
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Bcl-2 抑制剂

Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，拮抗所有抗凋亡Bcl-2家族蛋白（平均IC50，3 umol/L），包括Mcl-1（IC50，2.9 umol/L）和Bfl-1（IC50，5 umol/L）。了解更多

Product Citations (4)

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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
- Silva S, .et al. A diarylamine derived from anthranilic acid inhibits ZIKV replication, Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
- Chi-Hung R. Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells, Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
- P Geserick, .et al. The ratio of Mcl-1 and Noxa determines ABT737 resistance in squamous cell carcinoma of the skin, Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
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Pifithrin-u

Catalog No. A12449
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p53 抑制剂

Pifithrin-u通过降低p53与抗凋亡蛋白Bcl-2和Bcl-XL的亲和力来抑制p53与线粒体的结合。了解更多

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Amygdalin

Catalog No. A10074
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Amygdalin是最初从杏李的种子中分离的糖苷。苦杏仁苷通过调节人DU145和LNCaP前列腺癌细胞中Bax和Bcl-2的表达诱导凋亡。了解更多

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2-Methoxyestradiol

Catalog No. A10012
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Apoptotic, antiproliferative and antiangiogenic agent

2-Methoxyestradiol是一种凋亡，抗增殖和抗血管生成剂。通过两种途径诱导p53诱导的细胞凋亡：p38和NF-κB的激活；和激活JNK和AP-1导致Bcl-2磷酸化。了解更多

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