Organosulfur Compounds
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 Z-Phe-Arg-AFC
Chemical. CAS 93753-73-2 free base. Formula C33H33F3N6O6 . C2HF3O2. MW 666.7 . 114.0. Synthetic. Fluorogenic substrate, specifically used to determine the enzyme activity of Cathepsin L. Useful for the study of cathepsin activity and for screening small molecule inhibitors for drug discovery and HTS applications. Likely to be cleaved by cathepsins B, F, K, S and L, cathepsins L-like proteases and proteases such as papain, cruzipain, plasma kallikrein, soybean trypsin-like enzyme and the falcipains-1 and -2 malaria hemoglobinases. Hydrolysis of this substrate is monitored by observing fluorescence at an Excitation of 400nm and Emission at 505nm.
AdipoGen Indole-3-carbinol
Chemical. CAS 700-06-1. Formula C9H9NO. MW 147.2. Natural breakdown product of glucosinolates found in cruciferous vegetables. Widely used multifunctional aryl hydrocarbon receptor AhR agonist. AhR is emerging as a transcription factor involved in the regulation of both innate and adaptive immune responses in various immune cell types, including lymphocytes and antigen-presenting cells APCs. Studies have associated overexpression of AHR with the activation of cancer processes such as proliferation, epithelial-to-mesenchymal transition EMT, DNA damage, inflammation, migration and angiogenesis. Used to increase the population of innate lymphoid cells 3 ILC3 in gut microbiota. Chemopreventive agent that has multiple anticarcinogenic and antitumor properties and suppresses the proliferation of selective cancer cells, including breast cancer, prostate cancer, endometrial cancer, colon cancer and leukemic cells. Protects against nephrotoxicity. Proapoptotic.
AdipoGen RO-3306
Chemical. CAS 872573-93-8. Formula C18H13N3OS2. MW 351.5. Selective CDK 1 inhibitor Cdk1/B1 and Cdk1/A. Potential anti-cancer compound. Cell cycle arrest inducer at G1, S and G2/M . Apoptosis inducer in embryonic stem cells. Actively enhances downstream p53 signaling to promote apoptosis in AML cell lines. Suppresses phosphorylation of p53 at Ser315 and procaspase-8 at Ser387. Enhances Fas-mediated activation and processing of procaspase-8 in mitotic cells towards.
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.
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 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 Z-Leu-Leu-Glu-AMC
Chemical. CAS 348086-66-8. Formula C35H44N4O9. MW 664.8. Fluorogenic substrate for the peptidylglutamyl-peptide hydrolysing PGPH caspase-like activity of the 20S proteasome. Excitation 380nm. Emission 460nm.
AdipoGen Boc-Leu-Arg-Arg-AMC
Chemical. CAS 109358-46-5 free base. Formula C33H52N10O7 . C2H4O2. MW 700.8 . 60.1. Fluorogenic tri-peptide substrate for measuring the trypsin-like peptidase activity of the 20S proteasome. Substrate for the Kex2 endopeptidase from S. Cervisiae, which has substrate specificity toward the C-terminal side of LR, PR and RR sequences. Can be cleaved by Kallikrein 5 with a P1 site preference for basic residues R and K. Excitation 380nm. Emission 460nm. This substrate is useful for inhibitor screening and kinetic analysis.
AdipoGen Necrostatin-5 Nec-5
Chemical. CAS 337349-54-9. Formula C19H17N3O2S2. MW 383.5. Necroptosis inhibitor. Indirect RIP1 kinase inhibitor. Cardioprotective
AdipoGen Z-Leu-Leu-Phe-CHO
Chemical. CAS 133429-58-0. Formula C29H39N3O5. MW 509.7. Reversible and cell permeable proteasome inhibitor. Specifically inhibits the chymotrypsin-like activity of the proteasome. Calpain and cathepsin inhibitor. Does not inhibit the peptidyl-glutamyl peptide hydrolyzing activity of MPC.
AdipoGen Suc-Leu-Leu-Val-Tyr-AMC
Chemical. CAS 94367-21-2. Formula C40H53N5O10. MW 763.9. Fluorogenic substrate for measuring the chymotrypsin-like peptidase activity of the 20S proteasome, calpains and other chymotrypsin-like proteases. Extinction 380nm. Emission 460 nm. This substrate is useful for inhibitor screening and kinetic analysis.
AdipoGen Z-Leu-Leu-Leu-BOH2 MG-262
Chemical. CAS 179324-22-2. Formula C25H42BN3O6. MW 491.4. Highly potent and selective cell permeable inhibitor of the proteasome. Inhibits the chymotrypsin-like and caspase-like peptidase activity of the proteasome. Calpain and cathepsin inhibitor. Autophagy activator. Similar structure as MG-132 AG-CP3-0011 but much higher potency.
AdipoGen Z-Leu-Leu-Phe-CHO
Chemical. CAS 133429-58-0. Formula C29H39N3O5. MW 509.7. Reversible and cell permeable proteasome inhibitor. Specifically inhibits the chymotrypsin-like activity of the proteasome. Calpain and cathepsin inhibitor. Does not inhibit the peptidyl-glutamyl peptide hydrolyzing activity of MPC.
AdipoGen Ac-Arg-Leu-Arg-AMC
Chemical. CAS 929903-87-7 free base. Formula C30H46N10O6 . C2HF3O2. MW 642.8 . 114.0. Fluorogenic tri-peptide substrate for measuring the trypsin-like peptidase activity of the 20S proteasome. It is cleaved exclusively at the amide R-AMC bond to release fluorescent product. Shows low Km and high specific activity. Excitation 380nm. Emission 460nm. This substrate is useful for inhibitor screening and kinetic analysis.