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You are here:Home-Inhibitors & Agonists-Apoptosis-Bcl-2

Request The Product List ofBcl-2 Bcl-2

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, Bal-2, Bok, Mcl-1.



a) Schematic representation of BCL-2 family proteins identifying BCL-2 homology (BH) and transmembrane-targeting (TM) regions with respect to the BCL-2 core. At the left, the cartoons illustrate the structured, globular (rounded) or unstructured, intrinsically disordered (noodle-like) nature of the particular class of BCL-2 family proteins. The approximate position of α-helices in the BCL-2 core is marked at the bottom. Helices that delineate the BC groove are highlighted in red. b) The functional interaction network between pro- and anti-apoptotic BCL-2 family members is color coded as in panel a. c) The structure of the BCL-2 core of BCL-xL identifies the BH regions and α-helices colored as in panel a. d) A representative structure highlighting the BH3-into-BC groove interaction for the complex between BCL-xL and the BH3 region of BAD (shown in red). The conserved Leu and Asp side chains of BAD BH3 are engaged in hydrophobic and electrostatic interactions, respectively, with complementary sites in the BCL-2 core. PDB identifiers are shown at the bottom.


References:


1.Adams JM,et al. Science. 1998 Aug 28;281(5381):1322-6.

Cat. No. Product Name CAS No. Information
H9487

Lisaftoclax

 		2180923-05-9

Lisaftoclax is a novel, dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, Bcl-2/Bcl-xl inhibitor 1 exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively;First-in-human study of Lisaftoclax (APG-2575), in patients (pts) with relapsed/refractory (R/R) CLL and other hematologic malignancies (HMs).
H9422

(E)-GL0388

 		2640729-69-5

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM; GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
H9421

(Z)-GL0388

 		2640730-04-5

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM; GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
H9420

GL0388

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM; GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
H9087

WL 276

 		1042131-67-8

WL 276 is a small-molecule antagonist against anti-apoptotic Bcl-2 family proteins with IC50 value of 2.9 μM for Bcl-XL,overcomes drug resistance and suppresses prostate tumor growth.
H8959

Palcitoclax

 		1619923-36-2

Palcitoclax is a Bcl-X and Bcl-2 protein inhibitors.
H8955

Murizatoclax

 		2245848-05-7

Murizatoclax is a potent and selective MCL-1 inhibitor with IC50 values in the range of 0.000086 μM to 0.085 μM.
H8359

rel-CCT369260

 		2253878-44-1

rel-CCT369260 is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits a IC50 of 520 nM.
H8358

CCT369260

CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits a IC50 of 520 nM.
H1606

VU661013

 		2131184-57-9

VU661013 (VU-661013) is a novel potent, selective MCL-1 inhibitor with Ki of 97 pM (human MCL-1) in TR-FRET assay, shows no significant inhibition on BCL-xL (Ki>40 uM) or BCL-2 (Ki=0.73 uM); de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML, and is active in venetoclax-resistant cells and patient derived xenografts.

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