Bcl-2 Family Inhibitor

TC11 is a MCL1 degrader and apoptosis inducer. TC11 induces sustained CDK1 activation to phosphorylate and degrade MCL1, activates caspase-3, -8, and -9, inhibits centrosomal-regulatory NPM function to block centrosomal clustering, and triggers apoptosis independent of the cereblon pathway. TC11 blocks tumor cell proliferation in vitro and acts against tumor xenografts in vivo. TC11 can be used for the research of multiple myeloma.

NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC₅₀ of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease.

Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.

BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases.

Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC₅₀s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively. Sabutoclax increases Bax, Bim, PUMA and survivin expression.

VU661013 is a potent and selective MCL-1 inhibitor.

Difopein TFA is a 14-3-3 protein inhibitor. Difopein TFA acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein TFA serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein TFA is applicable to glioma-related research.

CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 (HY-10008) to BCL6 ligand BI3812 (HY-111381). CDK-TCIP1 potently and specifically kills BCL6-overexpressing cells with EC₅₀ of 7.7 nM for SUDHL5 cells.

Tegafur-gimeracil-oteracil potassium (S-1; TS-1) is an orally active anticancer agent composed of Tegafur (HY-17400), Gimeracil (HY-17469), and Oteracil potassium (HY-17511). Tegafur-gimeracil-oteracil potassium inhibits the proliferation, migration and invasion of endometrial cancer cells and induces apoptosis by blocking the PI3K/AKT/mTOR signaling pathway. Tegafur-gimeracil-oteracil potassium can be used in research related to endometrial cancer and gastric cancer with peritoneal metastasis.

Indole-3-pyruvic acid (Standard) is the analytical standard of Indole-3-pyruvic acid (HY-W028393). This product is intended for research and analytical applications. Indole-3-pyruvic acid is an orally active ketone analog of tryptophan, and is an aryl hydrocarbon receptor (AHR) agonist. Indole-3-pyruvic acid inhibits p38/MAPK phosphorylation, regulates the tryptophan metabolic pathway, and also possesses protective activities against skin photodamage, as well as anti-inflammatory and anti-anxiety bioactivities in the gut. Indole-3-pyruvic acid can downregulate the expression of IL-1β, IL-6, Cox-2, and Bax to alleviate UVB-induced keratinocyte toxicity. Indole-3-pyruvic acid can activate AHR to promote Tr1 cell differentiation, increase IL-10, and inhibit Th1 cytokine production. Indole-3-pyruvic acid can alter the levels of kynurenine metabolites in the brain, mediating central nervous system-related effects. Indole-3-pyruvic acid can be used in research on skin lesions, colitis, and anxiety.

Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection.

Secoxyloganin is an orally effective iridoid derivative. Secoxyloganin can be isolated from the flower buds of L. japonica. Secoxyloganin induces Apoptosis by inhibiting the expression of Bcl-2. Secoxyloganin potently inhibits the proliferation of breast cancer cells, while exerting weak activity against normal mammary epithelial cells. Secoxyloganin inhibits the decrease in tail vein blood flow associated with allergic reactions.

Gossypin is an orally active flavone isolated from Hibiscus vitifolius. Gossypin has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits AURKA and RSK2. Gossypin inhibits invasion and induces apoptosis. Gossypin can be used for gastric cancer study.

Secretoneurin, rat is a 33-amino acid neuropeptide produced by proteolytic processing of chromogranin II, widely distributed in the central and peripheral nervous systems, and its release is calcium-dependent. Secretoneurin, rat modulates the activities of caspase-3, caspase-1, the NLRP3 inflammasome, IGF-1R, VEGFR1, VEGFR2, FGFR3, AMPK, ERK1/2/MAPK, and Jak2/Stat3 pathways. Secretoneurin, rat regulates neuronal apoptosis, synaptic structure, inflammation, neurogenesis, angiogenesis, oxidative stress, cardiomyocyte hypertrophy, dopamine release, and cell migration and proliferation. Secretoneurin, rat is used in studies of global cerebral ischemia, myocardial infarction, stroke, and cardiac hypertrophy.

CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K_i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.

BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a K_i of 2.4±0.2 μM in FP assay. BH3I-1 has a K_d of 5.3 μM against the p53/MDM2 pair.

Simazine is a triazine herbicide. Simazine is widely used in agriculture, potted plant and tree production. In addition, Simazine can induce the apoptosis of immune cells in the spleen of mice and inhibit the proliferation of B cells and T cells in mice.

MCL-1/BCL-2-IN-2 is a Mcl-1 and Bcl-2 inhibitor with IC₅₀ values of 5.4 and 7.66 μM. MCL-1/BCL-2-IN-2 is applicable to the research of Mcl-1-dependent cancers.

Butyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research.

(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.