Signaling Pathway

Bcl-2 Family

Bcl-2 Family

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Bcl-2 is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, BAD, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). There are a total of 25 genes in the Bcl-2 family known to date. Human genes encoding proteins that belong to this family include: BAK1, BAX, BCL2, BCL2A1, BCL2L1, BCL2L2, BCL2L10, BCL2L13, BCL2L14, BOK, MCL1.

Bcl-2 Family Inhibitors & Modulators (27)

Product Name Catalog No. Brief Description
(+)-Apogossypol

HY-13408

(+)-Apogossypol(Apogossypol; NSC736630) is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM.

(S)-Gossypol acetic acid

HY-15464D

(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).

A-1155463

HY-19725

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-1210477

HY-12468

A-1210477 is an inhibitor of MCL-1 (Ki=0.45 nM in TR-FRET-binding assays), is a much weaker binder of BCL-2 (Ki=0.132 μM) and BCL-XL(Ki>0.660 μM).

ABT-199

HY-15531

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.

ABT-737

HY-50907

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.

AT-101

HY-15464

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.

AT-101 acetic acid

HY-15464A

AT101 acetic acid, 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.

BAM7

HY-15341

BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.

Bax inhibitor peptide V5

HY-P0081

Bax inhibitor peptide V5 is a peptide inhibitor of Bax translocation to mitochondria.

BH3I-1

HY-100383

BH3I-1 is an inhibitor of Bcl-xL with IC 50 of 293.95 μM.

Gambogic Acid

HY-N0087

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.

Gossypol

HY-13407

Gossypol has been known to exert a potential for anti-cancer, anti-inflammatory and other important therapeutic activities, gossypol binds and antagonizes anti-apoptotic effect of Bcl-2 family proteins.

Gossypol acetic acid

HY-17510

Gossypol-acetic acid, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic.

HA14-1

HY-12011

HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.

Laquinimod

HY-13010

Laquinimod (ABR-215062) is a potent immunomodulator.

Marinopyrrole A

HY-15613

Marinopyrrole (Maritoclax) is  a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 uM, >8 fold selectivity than BCL-xl (IC50 > 80 uM).

Mcl1-IN-1

HY-16669

Mcl1-IN-1 is a potent Mcl-1-selective inhibitor relative to the related Bcl-2 family protein Bcl-xL; demonstrated good Mcl-1 inhibition (IC50 = 2.4 uM) with no appreciable inhibition of Bcl-xL at 100 uM.

Mcl1-IN-2

HY-12826

Mcl1-IN-2 is a Mcl-1 inhibitor without reported IC50 value.

MIM1

HY-16695

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