|Description||Venetoclax is a small-molecule inhibitor that has high selectivity for Bcl-2 (Ki < 0.01 nM in cell-free assays) over Mcl-1. It suppresses anti-apoptotic Bcl-2, a protein commonly overexpressed in cancer cells, to induce programmed death of CLL cells. Venetoclax is used as a second-line treatment of chronic lymphocytic leukemia (CLL).|
|Current Developer||AbbVie; Genentech|
UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
Gossypol is an orally-active polyphenolic aldehyde with potential antineoplastic activity. Derived primarily from unrefined cottonseed oil, gossypol induces cel...
Mcl1-IN-2, a hydroxyquinoline derivative, is an Mcl-1 inhibitor.
BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.
Obatoclax mesylate is the mesylate salt of obatoclax, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and anti...
AT-101 acetic acid
AT101 acetic acid is orally bioavailable solvate of R-(-)-enantiomer of gossypol with potential antineoplastic activity. It is used as the treatment of non Hodg...
Pyridoclax, a pyridine derivative, has been found to be a Mcl-1 inhibitor that could induce apoptosis of cancer cells. IC50: 25 nM(Kd).
Venetoclax is a small-molecule inhibitor that has high selectivity for Bcl-2 (Ki < 0.01 nM in cell-free assays) over Mcl-1. It suppresses anti-apoptotic Bcl-2, ...
Bax inhibitor peptide V5
Bax inhibitor peptide V5, a peptide inhibitor, as a pro-apoptotic member of Bcl-2 family proteins and plays an important role in mitochondria-dependent apoptosi...
Marinopyrrole A, a new Mcl-1 inhibitor, could influence Mcl-1-Bim interaction and induce the degradation of Mcl-1 proteasomal and also lead to the apoptosis of ...
(S)-Gossypol acetic acid
(S)-Gossypol acetic acid, a Bcl-2 inhibitor, could effectively induce the death of Jurkat cells in which Bcl-2 or Bcl-xL is overexpressed. IC50: 18.1μM and 22.9...
BDA-366 is a BCL2-BH4 antagonist(Ki=3.3nM) which suppresses human myeloma growth. BDA-366 induces apoptosis in MM cell lines and primary MM cells by inducing BC...
MIM1 is a small molecule inhibitor of Mcl-1 (IC50= 4.8 uM) by selectively targets the BH3-binding pocket.
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.
WEHI-539, a selective BCL-XL inhibitor that can be function as a single-agent inducer of apoptosis while sparing normal cells, it leads to MOMP and apoptosis du...
Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM.
Gambogic acid is a natural product inhibitor of Hsp90.
Gossypol Acetic Acid
The Acetate acid salt form of gossypol which may represent a promising new anticancer agent with a novel molecular mechanism and warrants further investigation ...