Apoptosis Inducer

Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC₅₀=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (K_D(app) of 0.46 μM).

Alda-1 is a potent and selective ALDH2 agonist, which activates wild-type ALDH2 and restores near wild-type activity to ALDH2*2.

Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC₅₀s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.

Verbascoside is isolated from Acanthus mollis, acts as an ATP-competitive inhibitor of PKC, with an IC₅₀ of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.

Nitrochin (4-NQO) is a chemical carcinogen. Nitrochin induces oncostatin-M (OSM) in esophageal cells. Nitrochin induces DNA damage, and induces apoptosis via a p53-dependent mitochondrial signaling pathway.

OICR-9429, a chemical probe, is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .

AZD0156 is a potent, selective and orally active ATM inhibitor with an IC₅₀ of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.

Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.

RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC₅₀ of 27.4 μM.

Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC₅₀ value of 1.39 nM and functions as an extremely potent antagonist of XIAP.

Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.

Quercetin hydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.

Ginsenoside Rg1 is one of the major active components of Panax ginseng. Ginsenoside Rg1 ameliorates the impaired cognitive function, displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

Dextran sulfate sodium salt (DSS) (MW 35000-45000) is a polymer of dehydrated glucose with a molecular weight of approximately 35000-45000. DSS with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (DSS) (MW 35000-45000) is a potent inducer of colitis. Dextran sulfate sodium salt (DSS) (MW 35000-45000) can be used to induce model acute colitis, chronic colitis, and colitis-related colon cancer. Dextran sulfate sodium salt (DSS) (MW 35000-45000) may be related to macrophage dysfunction, intestinal flora dysbiosis, and is particularly toxic to the colonic epithelium.

Agatolimod ((ODN 2006; PF-3512676; CpG 7909)) is a TLR9 agonist and immunomodulator with an EC₅₀ of 180 nM against human TLR9. Agatolimod activates and upregulates the expression of both TLR9 and TLR6, and mediates downstream signaling pathways via IRAK4, IRF5, IRF7. Agatolimod induces Th1-type innate and adaptive immune responses, activates various immune cells and promotes antigen presentation, regulates antibody levels and immune cell infiltration, upregulates the secretion of multiple cytokines, induces apoptosis and cell cycle arrest, enhances cytotoxicity, and clears intracellular Salmonella. Agatolimod is applicable to research on COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis.

Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina.

Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.