Thioureas
AdipoGen Desacetylcolchicine tartrate
Chemical. CAS 49720-72-1. Formula C20H23NO5 . C4H6O6. MW 357.4 . 150.1. Synthetic. Anticancer colchicine analog. Microtubule polymerization inhibitor. Prevents cell division.
AdipoGen Josamycin
Chemical. CAS 16846-24-5. Formula C42H69NO15. MW 827.99. Synthetic. A member of the leucomycin family of macrolide antibiotics produced by Streptomyces kitasatoensis. May overcome anticancer drug resistance by inhibiting the binding of vinblastine or cyclosporin A to P-glycoprotein Pgp. An antimicrobial against a wide variety of pathogens.
AdipoGen GSH-OEt
Chemical. CAS 92614-59-0. Formula C12H21N3O6S. MW 335.38. Synthetic. GSH-OEt is cellpermeable and has been used to protect cells against radiation damage, oxidants and various toxic compounds including heavy metals. GSH-OEt is a protective agent against cellular damage, such as cataracts and mitochondrial degeneration. It undergoes hydrolysis by intracellular esterases thereby increasing intracellular GSH concentration in many tissues and cell types. Glutathione monoethyl ester may be used to supplement cellular pools of GSH in vitro and in vivo and can prevent ROS formation, neutralize toxic products and block apoptosis pathway. The effect of glutathione GSH and glutathione ethyl ester GSH-OEt supplementation on GSH homeostasis and exercise-induced oxidative stress was also examined. Glutathione ethyl ester protects against cisplatin-induced ototoxicity in the rat.
AdipoGen LY2835219
Chemical. CAS 1231930-82-7. Formula C27H32F2N8 . CH4O3S. MW 602.7. LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 CDK4 and CDK6 IC50s = 2 and 10 nM, respectively. Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.
AdipoGen 7-OH-4-methyl-21H-quinolone
Chemical. CAS 20513-71-7. Formula C10H9NO2. MW 175.18. Synthetic. 7-Hydroxy-4-methyl-21H-quinolone is a starting material for the synthesis of a potential cytotoxic compound class with activity against human tumor cell lines.
AdipoGen Josamycin
Chemical. CAS 16846-24-5. Formula C42H69NO15. MW 827.99. Synthetic. A member of the leucomycin family of macrolide antibiotics produced by Streptomyces kitasatoensis. May overcome anticancer drug resistance by inhibiting the binding of vinblastine or cyclosporin A to P-glycoprotein Pgp. An antimicrobial against a wide variety of pathogens.
AdipoGen Necrostatin-7 Nec-7
Chemical. CAS 351062-08-3. Formula C16H10FN5OS2. MW 371.4. Necroptosis inhibitor. Does not inhibit RIP1 kinase.
AdipoGen KBU2046
Chemical. CAS 1143863-69-7. Formula C15H11FO2. MW 242.2. Highly selective metastasis inhibitor in vitro. Binds to and stabilizes Cdc37-HSP90beta heterocomplexes, consequently blocking its function and inhibiting cancer cell motility. Does not bind to Cdc37 or HSP90beta alone. Inhibits cancer metastasis in vivo in murine models of human prostate and breast cancer. Shown to exhibit a complete lack of cellular cytotoxicity and systemic toxicity.
AdipoGen PK 11195
Chemical. CAS 85532-75-8. Formula C21H21ClN2O. MW 352.9. Selective peripheral benzodiazepine antagonist. Apoptosis enhancer. Glucose-induced insulin secretion inhibitor. Induces mitochondria cytochrome c release. Anticancer compound. Antiproliferative. Pharmacological tool in autophagy.
AdipoGen CTPB
Chemical. CAS 586976-24-1. Formula C31H43ClF3NO2. MW 554.1. Potent activator of p300 HAT histone acetyltransferase activity, which has an important role in regulation of gene expression. Does not show PCAF p300/CBP-associated factor HAT activities. Membrane-impermeable that requires a carrier to pass the membrane barrier of cells.
AdipoGen C646
Chemical. CAS 328968-36-1. Formula C24H19N3O6. MW 445.4. Reversible cell permeable p300/CBP histone acetyltransferase HAT inhibitor. Specific inhibition to p300 86% compared to N-acetyltransferase, PCAF, GCN5, Rtt109, Sas or MOZ histone acetyltransferases <10%. Cell growth inhibitor in melanoma and non-small-cell-lung NSCL human cancer cell lines.
AdipoGen PJ-34
Chemical. CAS 344458-15-7. Formula C17H17N3O2 . HCl. MW 295.2 . 36.5. Potent, water soluble polyADP-ribose polymerase PARP inhibitor. Inhibits peroxynitrite-induced cell necrosis. Shows significant, dose-dependent anti-inflammatory effects in a variety of local inflammation models. Provides cardioprotection by decreasing myocardial infarct size. Shows protective effects in models of stroke. Suppresses cell growth in liver cancer cells.
AdipoGen R-Roscovitine
Chemical. CAS 186692-46-6. Formula C19H26N6O. MW 354.5. Potent and selective inhibitor of CDKs. More potent than olomoucine. Inhibits CDK1/cyclin B kinase IC50 = 450 nM, CDK2 IC50 = 700 nM and CDK5/p35 IC50 = 160 nM. Inhibits M phase promoting factor MPF kinase activity. Arrests human fibroblasts in G1 phase. Antitumor compound. Activates the mitogen-activated protein kinase pathway. Targets both the p53 and NF-kappaB pathways10. Has effects on calcium channel gating. Prevents DNA damage-induced cyclin A1 upregulation. Apoptosis inducer. As CYC202 in phase I clinical trials. Reviews.
AdipoGen Alsterpaullone
Chemical. CAS 237430-03-4. Formula C16H11N3O3. MW 293.3. Potent CDK1/cyclin B IC50 = 35 nM inhibitor. Anti-tumor compound Potent inhibitor of CDK2/cyclin A, CDK2/cyclin E IC50 = 200 nM, CDK5/p25 IC50 = 40 nM, CDK5/p35 IC50 = 40 nM. GSK-3beta glycogen synthase kinase-3beta inhibitor. Apoptosis inhibitor. Apoptosis inducer. Angiogenesis inhibitor.
AdipoGen Z-Leu-Leu-Leu-AMC
Chemical. CAS 152015-61-7. Formula C36H48N4O7. MW 648.8. Fluorogenic substrate for measuring the chymotrypsin-like peptidase activity of the 20S proteasome. Excitation 345nm. Emission 445nm. This substrate is useful for inhibitor screening and kinetic analysis.