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Chemical. CAS 23465-76-1. Formula C22H27N3O2. MW 365.47. Synthetic. Quinoxaline compound, originally developed as a spasmolytic drug. Acts as an N-type calcium channel blocker, competitive AMPA receptor antagonist, and non-competitive NMDA receptor antagonist. Antioxidant agent through partial prevention of the formation and the highly active scavenging of hydroxyl radicals. Used to treat inner ear diseases such as tinnitus. Shown to inhibit tumor-promoting factors and potentially useful as a chemotherapeutic agent.
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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.
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Chemical. CAS 82571-53-7. Formula C13H12N2O2. MW 228.2. Synthetic. Ozagrel, an antithrombic drug, is a potent and selective TXA Synthase thromboxane A2 TXAS inhibitor. Acts as a selective inhibitor of TXAS with an IC50=11nM. The beneficial effects of TXAS inhibition by ozagrel include improved motor coordination after experimental stroke, and antihypertensive effects in spontaneously hypertensive rats.
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Chemical. CAS 167698-68-2 free base. Formula C34H44N8O8 . C2HF3O2. MW 692.8 . 114.0. Fluorogenic tetrapeptide substrate for ubiquitin C-terminal hydrolases UCHs, e.g. UCHL3 and isopeptidase T. LRGG is the preferred substrate sequence of the human deSUMOylating enzymes SENP6 and SENP7. Excitation 380nm. Emission 460nm.
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Chemical. CAS 63208-82-2. Formula C16H18N2OS . HBr. MW 286.4 . 80.9. p53 inhibitor. Reversibly blocks p53-dependent transcriptional activation. Tool to combat side effects of cancer therapy. Apoptosis inhibitor.
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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.
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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.
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SEIT is a potent inhibitor of NOS in vitro but lacks good in vivo efficacy due to poor cellular penetration. The Ki values are 19, 39, and 29 nM using purified human iNOS, eNOS, and nNOS, respectively.{1292,1351,2259}
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S-Isopropylisothiourea hydrobromide is a small-molecule inhibitor targeting nitric oxide synthase (NOS) It is designed to inhibit NOS activity thereby reducing nitric oxide (NO) production and modulating NO-mediated biological processes S-Isopropylisothiourea hydrobromide exerts its biological activity primarily through selective NOS inhibition Based on these pharmacological properties S-Isopropylisothiourea hydrobromide holds research potential in investigating NO-related processes particularly in pathophysiological contexts such as hemorrhagic shock
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