Bcl-2

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Bcl-2 Inhibitors | Activators (11)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
  • Nat Biotechnol, 2011, 29(6):542-6
  • Nat Med, 2013, 19(11):1478-88
  • Mol Cell, 2012, 46(5):573-83
S1001 ABT-263 (Navitoclax) ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM, but binds more weakly to Mcl-1 and A1. Phase 2.
  • J Clin Invest, 2014, 124(1):117-28
  • J Clin Invest, 2014, 124(11):4737-52
  • Proc Natl Acad Sci U S A, 2014, 111(41):14788-93
S1057 Obatoclax Mesylate (GX15-070) Obatoclax (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.
  • Cancer Res, 2012, 72(12):3069-79
  • Cancer Res, 2011, 71(13):4494-505
  • Oncogene, 2012, 32(37):4331-42
S1121 TW-37 TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.
  • Cell Death Differ, 2013, 20(11):1475-84
  • Cell Death Differ, 2012, 19(12):1896-907
  • Mol Oncol, 2015, 9(2):409-21
S8048 ABT-199 (GDC-0199) ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.
  • Cell Death Differ, 2014, 21(7):1170-7
  • Cell Death Differ, 2014, 21(12):1877-88
  • J Biol Chem, 2014, 289(23):16190-9
S7531 UMI-77 UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
S8061 Sabutoclax Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
S2812 AT101 AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID. Phase 2.
  • Drug Des Devel Ther, 2014, 8:2517-29
S1071 HA14-1 HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.
  • Cancer Res, 2011, 71(13):4494-505
  • J Biol Chem, 2014, 289(38):26481-91
S7105 BAM7 BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2448 Gambogic Acid Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.
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Tags: Bcl-2 apoptosis | Bcl-2 inhibition | Bcl-2 protein | Bax apoptosis | Bak protein | Bax protein | Bcl-2 cancer | Bcl-2 expression | Bcl-2 lymphoma | Bcl-2 protein family | Bak apoptosis | Bcl-2 pathway | Bcl-2 phosphorylation | Mcl-1 apoptosis | Bcl-xL apoptosis | Bcl-2 apoptosis pathway | Bcl-2 activation | Bcl-xL protein | Bcl-2 cleavage | Bcl-2 inhibitor clinical trial | Bcl-2 inhibitor review
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