Bcl-2 Family

Thevetiaflavone could upregulate the expression of Bcl?2 and downregulate that of Bax and caspase?3.

Mcl1-IN-2 is a selective Mcl-1 inhibitor.

Mcl1-IN-1 is a potent and selective inhibitor of the apoptosis regulating proteins Mcl-1.

Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.

Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.

PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

NPB is a specific and potent inhibitor of BAD phosphorylation at Ser99, with an IC50 of 0.41 μM.

Mcl-1 antagonist 1 is a Mcl-1 protein antagonist extracted from patent WO2019173181, compound 200.

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.

Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.

dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.

Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.

MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.

(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.

Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells.

MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.

Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.

BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively.

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

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.

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.

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.

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.

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.

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.