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.

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.

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.

(E)-Ferulic acid ((E)-Coniferic acid) causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin.t(E)-Ferulic acid exert both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.

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).

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki IC50: 0.454 26.2 nM).

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

UMI-77 is a selective Mcl-1 inhibitor. UMI-77 binds to the BH3-binding groove of Mcl-1 with a Ki of 490 nM and is selective over other members of the Bcl-2 family.

BDA-366, a potent Bcl2 antagonist, selectively binds the Bcl2-BH4 domain with high affinity (Ki = 3.3 nM), inducing a conformational change that nullifies its antiapoptotic function, thereby transforming it into a pro-apoptotic entity. This compound effectively suppresses lung cancer cell growth[1].

S55746 (BLC201) is an effective and selective BCL-2 inhibitor (Ki: 1.3 nM and a Kd of 3.9 nM).

Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

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.

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.

MIK665 (S-64315) (S-64315) has an inhibitory effect on myeloid leukemia.

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

Thymoquinone (NSC 2228) is a compound be found in herbs and spices with anti-inflammatory and anti-oxidant effects.

Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor exhibiting anticancer activity.

Ergosta-4,6,8(14),22-tetraen-3-one exhibits cytotoxic activity against human gastric cancer cells and can induce G2 M cell cycle arrest and apoptosis in human hepatocellular carcinoma (HepG2) cells. These findings could facilitate the further use of various medicinal fungi in cancer treatment.

BRD-K20733377 is a Bcl-2 inhibitor that exhibits selective cytotoxicity toward senescent cells, specifically inhibiting the activity of etoposide-induced senescent IMR-90 cells with an IC50 of 10.7 μM. Additionally, BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21, and KI67 in aged mouse models.

BM-962 (Compound 31) is a potent small-molecule inhibitor with an IC50 value of 4 nM (Ki=0.8 nM) for Bcl-2 and an IC50 of 3.9 nM (Ki<1 nM) for Bcl-xL. It inhibits H1417 and H146 cell lines with IC50 values of 9 and 13 nM, respectively, and shows potential for use in cancer research.

Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.

TS-IN-5 (Compound 15) is an inhibitor of thymidylate synthase (TS). It induces apoptosis by modulating the proteins Bax, BCL-2, PI3K, and STAT1. TS-IN-5 exhibits antitumor activity against liver cancer, breast cancer, and colon cancer.