Bcl-2

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1002 ABT-737 <1 mg/mL 100 mg/mL <1 mg/mL
S1001 Navitoclax (ABT-263) <1 mg/mL 100 mg/mL <1 mg/mL
S1057 Obatoclax Mesylate (GX15-070) <1 mg/mL 83 mg/mL <1 mg/mL
S1121 TW-37 <1 mg/mL 115 mg/mL 4 mg/mL
S8048 Venetoclax (ABT-199, GDC-0199) <1 mg/mL 100 mg/mL <1 mg/mL
S8383 S63845 100 mg/mL
S7100 WEHI-539 -1 mg/mL 100 mg/mL -1 mg/mL
S8591 FX1 <1 mg/mL 73 mg/mL <1 mg/mL
S7126 Marinopyrrole A (Maritoclax) <1 mg/mL 100 mg/mL 45 mg/mL
S8177 BH3I-1 <1 mg/mL 64 mg/mL 13 mg/mL
S7849 BDA-366 <1 mg/mL 84 mg/mL 5 mg/mL
S2812 AT101 <1 mg/mL 116 mg/mL 89 mg/mL
S1071 HA14-1 <1 mg/mL 82 mg/mL 82 mg/mL
S7105 BAM7 <1 mg/mL 2 mg/mL <1 mg/mL
S8061 Sabutoclax <1 mg/mL 100 mg/mL 54 mg/mL
S7790 A-1210477 <1 mg/mL 3 mg/mL <1 mg/mL
S2448 Gambogic Acid <1 mg/mL 100 mg/mL 100 mg/mL
S7800 A-1155463 <1 mg/mL 80 mg/mL 100 mg/mL
S7801 A-1331852 <1 mg/mL 100 mg/mL <1 mg/mL
S7531 UMI-77 <1 mg/mL 93 mg/mL 93 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
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 in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

S1001

Navitoclax (ABT-263)

Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.

S1057

Obatoclax Mesylate (GX15-070)

Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.

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 in cell-free assays, respectively.

S8048

Venetoclax (ABT-199, GDC-0199)

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

S8383New

S63845

S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.

S7100New

WEHI-539

"WEHI-539 has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members."

S8591New

FX1

FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases.

S7126New

Marinopyrrole A (Maritoclax)

Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.

S8177New

BH3I-1

BH3I-1 is a Bcl-XL-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.

S7849New

BDA-366

BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity.

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 in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2.

S1071

HA14-1

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

S7105

BAM7

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

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.

S7790

A-1210477

A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

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.

S7800

A-1155463

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

S7801

A-1331852

A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases.

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.

Catalog No. Information Product Use Citations Product Validations
A5010New

Bcl-2 Rabbit Recombinant mAb

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