Bcl-2 Family

Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.

BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM.

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.

WEHI539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.

WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM.

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

AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).

Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).

Bax inhibitor peptide, negative control, negative control peptide for the Bax inhibitor peptides V5 and P5 , which inhibit Bax translocation to mitochondria and Bax-mediated apoptosis in vitro.

Muristerone A is a phytoecdysteroid analog of ecdysone which induces genes in mammalian cells and causes apoptosis in cells transfected with wild-type Bax.

BDA-366 selectively inhibits BCL2, converting it to a cell death inducer.

A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki = <0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM)

A-1331852 is a potent and selective BCL-XL inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML.

AZD-4320 is a BH3 mimetic and dual Bcl-2/Bcl-XL inhibitor.

S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity.

MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.

MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.