9 products were found matching "Cay14645"!

beta-Secretase 1 (BACE1) is an aspartic protease and member of the peptidase A1 protease family. BACE1 is transcribed as a preprotein composed of an N-terminal signal peptide, a pro-peptide, a catalytic domain, a transmembrane domain, and a cytosolic domain. The N-terminal signal peptide traffics the BACE1...

Caspase-3/7 inhibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (Ki(app) = 60 nM, IC50 = 120 nM) and caspase-7 (Ki(app) = 170 nM). It is a weaker inhibitor of caspase-9 (Ki(app) = 3.1 µM) and caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8 (Ki(app)s >25 µM). Caspase-3/7...

NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/KCa3.1, IC50 = 9.4 nM in HEK293 cells expressing the human channel). It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Cay-11016) (IC50s = 14, 15, and 9...

JWH 018 (Cay-10900) is a mildly selective agonist of peripheral cannabinoid (CB2) receptor, derived from the aminoalkylindole WIN 55,212-2. JWH 018 binds central cannabinoid (CB1) and CB2 receptors with Ki values of 9.0 and 2.94 nM, respectively. JWH 018 is one of several synthetic CBs that have been included in...

Lonidamine, originally identified as a potent antispermatogenic agent, inhibits glycolysis though the inactivation of mitochondria-bound hexokinase. It can decrease oxygen consumption as well as aerobic and anaerobic glycolysis in Ehrlich ascites tumor cells with IC50 values of 90 and 45 µM, respectively. A role for...

Myoseverin is a trisubstituted purine which binds microtubules, reversibly altering cellular function. At 20 µM, it directly binds tubulin and disrupts the structure of the microtubule cytoskeleton, resulting in myotube fission. Myoseverin arrests cell cycle in the G2/M phase, followed by DNA synthesis and cell...

Maraviroc is an antagonist of chemokine (C-C motif) receptor 5 (CCR5, Ki = 0.24 nM for the rhesus monkey recombinant receptor). It inhibits binding of MIP-1alpha, MIP-1beta, and RANTES to HEK293 cell membranes expressing CCR5 (IC50s = 3.3, 7.2, and 5.2 nM, respectively) and inhibits HIV-1 binding to CCR5 via...

Aloesin is a C-glycosylated chromone compound found in aloe (Liliaceae) that inhibits tyrosinase (IC50 = 0.9 mM), an enzyme responsible for catalyzing the first step of the conversion of tyrosine to melanin. Derivatives of aloesin have been shown to exhibit free radical scavenging and anti-inflammatory activity. The...

Human sirtuin 2 (SIRT2) is a NAD+-dependent protein deacetylase with diverse targets, including alpha-tubulin, phosphoenolpyruvate carboxykinase, and forkhead box protein O1. JFD00244 is an inhibitor of SIRT2 (IC50= 56.7 µM). At 5 µM, JFD00244 induces granulocytic differentiation in the acute promyelocytic leukemia...