Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model[1][2].
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL)[1][2].
Lenalidomide hydrochloride is a potent inhibitor of TNF-α and has antiangiogenic effect. Lenalidomide functions as a protein homeostatic modulator (PHM) linking casein kinase 1A1 (CKIα) to the human E3 ligase cereblon.
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALKL1196M and ALKG1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research[1].
Lorlatinib-d3 is the deuterium labeled Lorlatinib. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M
Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity[1].
Artonin E (5'-Hydroxymorusin) is a known prenylated flavonoid that induces apoptosis and arrests the cell cycle in S phase. Artonin E can induce anti-proliferative effects through mitochondrial pathway dysregulation and can be used in cancer research[1].
Lapatinib-d7 (GW572016-d7) ditosylate is the deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].
M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability[1].
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
α-Vitamin E-d9 is the deuterium labeled α-Vitamin E[1]. α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant[2][3].
CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-?B and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis[1].
Mcl-1 inhibitor 9 (example 2) is a myeloid cell leukemia 1 (Mcl-1) inhibitor with IC50 value of 0.21889 nM. Mcl-1 inhibitor 9 shows anti-tumor activity[1].
Bcl-2-IN-12 (Compound 1) is a Bcl-2 inhibitor (IC50: 6 nM). Bcl-2-IN-12 can be used for cancer research[1].
Thrombospondin-1 (1016-1023) (human, bovine, mouse), is the C-terminal end of the native sequence of Thrombospondin-1 (TSP-1), is a CD47 agonist peptide[1].
Borrelidin (Treponemycin) is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei, which acts as an inhibitor of bacterial and eukaryal threonyl-tRNA synthetase, can target ALL cell lines by inducing apoptosis and mediating G(1) arrest. Borrelidin (Treponemycin) is an inhibitor of a cyclin-dependent kinase (CDK) of the budding yeast, Cdc28/Cln2 with an IC50 of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor with an IC50 of 0.8 nM for capillary tube formation, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum[1][2][3].
Ac-YVAD-AOM is the inhibitor of caspase-1 that shows antitumor activity[1].
Verubulin (MPC-6827) is a microtubule-disrupting agent with potent and broad-spectrum in vitro and in vivo cytotoxic activities, and acts as a promising candidate for the treatment of multiple cancer types[1].
Caspase-8-IN-1 is a potent caspase-8 inhibitor[1].
Z-LEED-FMK is a caspase-13 and caspase-4 inhibitor. Z-LEED-FMK also inhibits caspase-1 processing in S. typhimurium-infected macrophages[1][2].
Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) induces hepatocyte apoptosis[1][2].
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].
YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner[1].
CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis[1].
Curcumin 5-8 (CUR5-8) is a potent and orally active naturally active curcumin (CUR) analog. Curcumin 5-8 inhibits lipid droplet formation. Curcumin 5-8 increases autophagy and inhibits Apoptosis. Curcumin 5-8 improves insulin resistance and insulin sensitivity[1].
Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrial membrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research[1].
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].
Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability[1][2].
Tubulysin M is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. Tubulysin M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].
Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis[1].