bcl-2 family

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Navitoclax (ABT-263) is a potent oral Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM), demonstrating antitumor activity and inducing apoptosis.

Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces autophagy and apoptosis.

S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

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

MIK665 (S-64315) is a small-molecule inhibitor and a myeloid cell leukemia sequence 1 (MCL1) inhibitor (IC50 = 1.81 nM) with high selectivity and cell permeability. Used in experimental research, this compound exhibits antitumor activity in hematologic malignancies such as acute myeloid leukemia.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

Semaglutide Acetate is a GLP-1R agonist (EC50=6.2 pM) with long-acting, selective, competitive, and oral efficacy. Semaglutide acetate can be used in the study of type 2 diabetes.

Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA) analog and an agonist of TLR3 as well as retinoic acid-inducible gene I (RIG-I) and melanoma differentiation-associated protein 5 (MDA5). It can induce innate immune responses in mammals and serve as a vaccine adjuvant to enhance both innate and adaptive immunity, while modulating the tumor microenvironment and directly inducing apoptosis in cancer cells. Poly(I:C) is commonly used to establish acute respiratory distress syndrome (ARDS) animal models for studying immune responses and disease mechanisms.

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.

Bz 423 is a potent immunomodulator that induces apoptosis by activating Bax and Bak to induce mitochondrial outer membrane permeabilization and cytochrome c release.Bz 423 shows partial activity in a mouse model of lupus.

Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic leukemia and non-Hodgkin's lymphoma.

Sonrotoclax is a potent, orally active inhibitor of Bcl2, demonstrating effective cell-killing activity against a range of lymphoma and leukemia cell lines [1].

TV 3279 is a novel ChE-MAI inhibitor , and the neuroprotective properties depend on their ability to induce the anti-apoptotic proteins PKC, Bcl-2, Bcl-x, and SOD, and to block the nuclear translocation of the pro-apoptotic enzyme glyceraldehyde phosphate dehydrogenase in PC-12 and neuroblastoma cells.

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

BFC1108 targets Bcl-2 and converts it to a pro-apoptotic protein, inhibits the growth of triple-negative breast cancer xenografts with high Bcl-2 expression, inhibits breast cancer lung metastasis, and induces apoptosis of Bcl-2-expressing cancer cells.

ARV-393 HCl is an orally active and potent PROTAC targeting BCL6 with antitumor activity for the study of non-Hodgkin's lymphoma.

SMBA1 is a highly potent Bax agonist with antitumor activity that induces cell cycle arrest and apoptosis in malignant glioma cells. SMBA1 can be used to study triple-negative breast cancer.

PF-07328948 is a branched-chain keto acid dehydrogenase kinase (BDK) inhibitor, useful in research on cardiovascular disease (CVD) and metabolic disorders.

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

BT2, a BCKDC kinase (BDK) inhibitor, exhibits an IC50 of 3.19 μM and functions as a potent, selective Mcl-1 inhibitor with a Ki value of 59 μM. Its interaction with BDK induces helix movements in the N-terminal domain, leading to BDK's dissociation from the branched-chain α-ketoacid dehydrogenase complex (BCKDC).

Gossypol acetic acid (AT101), a polyphenolic compound isolated from cottonseeds, binds with Bcl-2, Bcl-xL, Mcl-1, and does not inhibit BIR3 domain and BID.