Apoptosis Inducer

Rabeprazole-d₄ potassium is deuterated labeled Rabeprazole potassium. Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an b>IC₅₀ of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.

c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC₅₀ value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner.

ZNF281-IN-1 is a ZNF281 inhibitor. ZNF281-IN-1 disrupts the binding of transcriptionally active DNA-bound ZNF281 to the promoters of target genes including TRIM35 and ZEB1. ZNF281-IN-1 inhibits tumor cell proliferation, stabilizes P53 and upregulates PUMA to induce apoptosis, while triggering cellular senescence. ZNF281-IN-1 completely prevents Doxorubicin (HY-15142A)-induced cardiotoxicity (AIC), and enhances rather than impairs the antitumor efficacy of Doxorubicin. ZNF281-IN-1 completely blocks the distant metastasis of melanoma to the lungs. ZNF281-IN-1 can be used in the research of cardiotoxicity, lung cancer and metastatic melanoma.

IMB5046 is a microtubule inhibitor that induces apoptosis by blocking the G2/M phase of the cell cycle. IMB5046 has anti-tumor activity.

Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the K_d values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction.

Chlamydocin (purity≥70%), a fungal metabolite, is a highly potent HDAC inhibitor, with an IC₅₀ of 1.3 nM. Chlamydocin (purity≥70%) exhibits potent antiproliferative and anticancer activities. Chlamydocin (purity≥70%) induces apoptosis by activating caspase-3.

PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) (IC₅₀=0.35 μM). PRDX1-IN-2 decreases the mitochondria membrane potential of SW620 cells, probably due to ROS induced by PRDX1 inhibition, leading to cell apoptosis. PRDX1-IN-2 can be used for colorectal cancer research.

TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC₅₀ values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA^G595R, TRKA^F589L, and TRKA^G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells.

ODZ10117 is a STAT3 and NLRP3 inhibitor with a human STAT3 SH2 domain IC₅₀ of 7.5 μM. ODZ10117 binds to the STAT3 SH2 domain, suppressing tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity. ODZ10117 binds to NLRP3, impairs NEK7 interaction, prevents inflammasome formation, and inhibits caspase-1 and IL-1β cleavage.ODZ10117 reduces MSU (HY-B2130A)-induced IL-1β release, lowers LPS (HY-D1056)-induced sepsis mortality, and exhibits anti-inflammatory effects. ODZ10117 induces apoptosis, suppresses breast cancer cell migration and invasion, reduces tumor growth and lung metastasis, and extends survival in breast cancer models. ODZ10117 can be used for the research of Monosodium urate (HY-B2130A)-induced peritonitis, LPS-induced sepsis, breast cancer, glioblastoma, and Alzheimer's disease.

PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC₅₀ = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma.

Les-6666 is a β-tubulin inhibitor. Les-6666 exerts antiproliferative, pro-apoptotic, cell cycle arrest and migration-inhibitory effects, and suppresses DNA synthesis. Les-6666 can be used in the research of pancreatic cancer.

Isatin (Standard) is the analytical standard of Isatin. This product is intended for research and analytical applications. Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM). Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity. Shows effect on the serotonergic system.

Tambulin is an orally active flavonol compound found in Zanthoxylum armatum. Tambulin can inhibit cell proliferation, induce apoptosis and inhibit ROS production. Tambulin upregulates cleaved caspase-3, cleaved caspase-9, and Bax, downregulates Bcl-2 levels. Tambulin can stimulate glucose-dependent insulin secretion and induce endothelium-independent vasorelaxation. Tambulin binds to succinate dehydrogenase (SDH) (Ki = 11.02 μM) and shows significant ferric reducing power. Tambulin can enhances oxidative stress resistance, reduces, lipofuscin deposits, lipid levels, α-synuclein levels, improves locomotary behavior, and dopamine levels in in age-synchronized L1 hermaphrodite Caenorhabditis elegans models of ageing and Parkinson's disease. Tambulin can be used for the researches of Parkinson's disease, lung squamous cell carcinoma, and diabetes.

Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of E3 ligase and linker for the synthesis of Aster-A PROTAC degrader (HY-D2336).

EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR^WT, EGFR^T790M, COX-1 and COX-2 with IC₅₀s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC₅₀s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC₅₀s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects.

HDAC1-IN-11 (Compound 6) is a HDAC1 inhibitor with an IC₅₀ of 106.6  nM. HDAC1-IN-11 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC1-IN-11 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC1-IN-11 can be used for chemotherapy of cancers like NSCLC research.

Caspase-3 activator 4 (compound 4o) is a potent and cross the blood-brain barrier caspase-3 activator. Caspase-3 activator 4 shows antiproliferative activity. Caspase-3 activator 4 induces apoptosis. Caspase-3 activator 4 increases the gene expression of TNF-α. Caspase-3 activator 4 decreases the protein expression of cleaved caspases 3/caspases 3.

ChoKα inhibitor-5 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-5 can inhibit HChoK α1 with an IC₅₀ value of 0.64 μM. ChoKα inhibitor-5 also can induce apoptosis. ChoKα inhibitor-5 can be used for the research of cancer.

PPM-18 (NSC 73233) is a Vitamin K (HY-B2172) analog. PPM-18 prevents LPS-induced IκBα degradation, thereby inhibiting NF-κB activation and nuclear translocation of NF-κB. PPM-18 inhibits LPS-induced nitrite production and iNOS expression. PPM-18 inhibits HDAC6. PPM-18 induces ROS accumulation, activates AMPK, inhibits the mTORC1 and PI3K/AKT pathways, initiates Autophagy, and induces Apoptosis. PPM-18 suppresses seizures in zebrafish and mouse epilepsy models. PPM-18 prevents LPS-induced lethal toxicity and delayed hypotension. PPM-18 exhibits anticancer activity against leukemia and bladder cancer. PPM-18 can be used in research related to septic shock, bladder cancer and atherosclerosis.

Anti-CCL2 (Carlumab)-VcMMAE is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated with valine-citrulline (vc) and the tubulin inhibitor MMAE (HY-15162). The ADC toxic molecule and linker part are McMMAE (HY-15575). Anti-CCL2 (Carlumab)-VcMMAE induces apoptosis and can be used in cancer research.