Bcl-2 Family

ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).

Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).

TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer mediated through a novel pathway involving inactivation of Notch-1 and Jagged-1.

HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2.

Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. 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.

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.

ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.

BAM 7 binds the BAX trigger site with an EC50 ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX.

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).

UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.

Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic.

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32μM, 0.48μM and 0.18μM.

Bax inhibitor peptide P5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro.

Bax inhibitor peptide V5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro.

A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines.

BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL

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)

CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).

MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 μM) that overcomes Mcl-1-dependent leukemia cell survival.

(S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM).

Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM.

BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.

FX1 is an inhibitor of the transcription factor B cell lymphoma 6 (BCL6) with IC50 value of ~35 μM.

Marinopyrrole A, aslo known as Maritoclax, is a selective inhibitor of Mcl-1 with IC50 value of 10.1μM.

BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM.

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.

ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction

TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR.

(E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.

Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic drugs.