Thioureas
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 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 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 1-Azakenpaullone
Chemical. CAS 676596-65-9. Formula C15H10BrN3O. MW 328.2. Potent and ATP-competitive GSK-3beta glycogen synthase kinase-3beta inhibitor IC50 = 18 nM.
AdipoGen SB202190
Chemical. CAS 152121-30-7. Formula C20H14FN3O. MW 331.3. Potent and cell permeable p38 MAP kinase inhibitor. Apoptosis inducer. Inhibits p38alpha and beta, but not gamma and delta isoforms. Does not inhibit ERK2 or other members of the MAP kinase family or their upstream activators. JNK activator. Autophagic vacuole inducer
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 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 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 MTSSL
Chemical. CAS 81213-52-7. Formula C10H18NO3S2. MW 264.3. Highly reactive, thiol-specific spin-label. Specific conformational probe of thiol site structure by its minimal rotational freedom and distance from the covalent disulfide linkage to the macromolecule under study. Used to label cysteine residues in proteins site-directed labeling, SDS-labeling. Allows protein structure and protein dynamics determination as well as the study of protein-protein and protein-oligonucleotide interactions.
AdipoGen Carboplatin
Chemical. CAS 41575-94-4. Formula C6H12N2O4Pt. MW 371.3. Potent platinum-based antineoplastic agent. Analog of cisplatin Prod. No. AG-CR1-3590 with reduced nephrotoxicity and higher stability. Antitumor agent. Forms inter- and intrastrand DNA adducts/crosslinks, consequently blocking DNA replication and transcription and inducing cell death. Interferes with cell division by mitosis. The damaged DNA elicits DNA repair mechanisms, which in turn activate apoptosis when repair is impossible. Apoptosis inducer. Enhances radiation-induced single-strand DNA breakage.
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 1-Azakenpaullone
Chemical. CAS 676596-65-9. Formula C15H10BrN3O. MW 328.2. Potent and ATP-competitive GSK-3beta glycogen synthase kinase-3beta inhibitor IC50 = 18 nM.
AdipoGen Efavirenz
Chemical. CAS 154598-52-4. Formula C14H9ClF3NO2. MW 315.7. Efavirenz is a non-nucleoside reverse transcriptase inhibitor NNRTI that exhibits antiviral and anticancer activities. Efavirenz binds to wild-type and mutant HIV-1 RTs Ki= 2.93nM and 3.85-56.5nM, respectively. It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells IC95s = 1.5-1,500 nM. Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17nM. Efavirenz is an anti-HIV drug, commonly used in combination therapy for AIDS treatment. It is part of highly active antiretroviral therapy HAART for the treatment of a human immunodeficiency virus HIV type 1. In various cancer cell lines, Efavirenz inhibits cellular proliferation and increases activation of p53. CARD8 inflammasome senses HIV-1 protease activity. In HIV1-infected cells, CARD8 cannot detect the virus because the viral protease remains inactive as a subunit of unprocessed Gag-Pol polyprotein.