Bcl-2 Family

Bax-activator-106 is a specific Bax agonist. It acts by promoting Bax-dependent but not Bak-dependent apoptosis.

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

LTX-315 is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.

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

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.

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

Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with

(+)-Apogossypol 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 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.

AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay.

AZD-5991 Racemate is the racemate of AZD-5991. AZD-5991 Racemate is a Mcl-1 inhibitor with an IC50 of <3 nM in FRET assay.

AZD-5991 S-enantiomer is the less active enantiomer of AZD-5991. AZD-5991 S-enantiomer is a Mcl-1 inhibitor with an IC50 of 6.3 μM in FRET assay and a Kd of 0.98 μM in surface plasmon resonance (SPR) assay.

BI-3802 is a highly potent BCL6 degrader, inhibiting the BTB domain of BCL6, with an IC50 of ??3 nM; BI-3802 has antitumor activity.

Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively.

BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ??3 nM; BI-3812 has antitumor activity.

Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes. Lobaplatin (D-19466) shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent.

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.

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.

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

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.

Bz-423 is an F1F0-ATPase modulator. It acts by selectively killing autoimmune lymphocytes.

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

DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology.

BM-1244 is a selective inhibitor of Bcl-xL and Bcl-2, exhibiting Ki values of 134 nM and 450 nM, respectively. This compound induces apoptosis and suppresses tumor growth through the release of cytochrome C and Smac from mitochondria, leading to caspase-3 activation and PARP cleavage. BM-1244 has demonstrated synergistic effects with chemotherapy in vivo, making it a valuable research tool for studying colorectal cancer, acute myeloid leukemia, and gastric cancer.

Pelcitoclax is a potent inhibitor of Bcl-2 and Bcl-xl, designed to induce apoptosis in cancer cells. Its primary mechanism involves disrupting the anti-apoptotic activity of these proteins, leading to increased cell death in malignant tissues. Pelcitoclax is utilized in research to explore therapeutic strategies against various malignancies and to study apoptotic pathways in cellular models.

Lisaftoclax is a potent inhibitor of the anti-apoptotic proteins Bcl-2 and Bcl-xl. With IC50 values of 2 nM for Bcl-2 and 5.9 nM for Bcl-xl, Lisaftoclax demonstrates significant anti-tumor activity. This compound is primarily utilized in research focused on cancer therapy, particularly in studies exploring mechanisms of apoptosis and the role of Bcl-2 family proteins in tumor survival.

AS1411 (AGRO-100) is a G-rich oligonucleotide aptamer that selectively targets nucleolin, a nucleoprotein overexpressed on the surface and within the nucleus of many cancer cells. It inhibits tumor cell proliferation by disrupting nucleolin-containing complexes, thereby affecting key oncogenic processes. AS1411 has been shown to reduce PRMT5 expression and inhibit tumor growth in DU145 prostate cancer cells, and to block the interaction between nucleolin and *bcl-2* mRNA in MCF-7 breast cancer cells, leading to decreased Bcl-2 protein levels and enhanced apoptosis. Beyond its intrinsic anticancer activity, AS1411 serves as a precision-targeting carrier for the delivery of nanoparticles, oligonucleotides, and small molecules to cancer cells. AS1411-conjugated gold nanospheres have demonstrated effective inhibition of breast cancer cell proliferation in vitro and in vivo, with the added advantage of crossing the blood-brain barrier and exhibiting low tissue toxicity, making AS1411 a versatile platform for targeted cancer therapy and drug delivery.