16 products were found matching "Cay13482-%25"!

MS-275 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 µM). However, it does not inhibit HDAC8 (IC50 > 100 µM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in...

Puromycin is a derivative of the glomerular epithelial cell toxin puromycin aminonucleoside (Cay-15509) and an inhibitor of protein synthesis that has been found in S. alboniger. Puromycin is structurally similar to the amino acid-bearing end of tRNA, which allows it to enter the ribosome during protein synthesis,...

STF-62247 is a small molecule agonist that induces autophagy and selectively causes lethality in renal cell carcinoma (RCC) cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 nM). It significantly reduces the growth rate of tumors formed from VHL-deficient cells in mice. STF-62247...

Equol is a nonsteroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzein by human intestinal microflora. The estrogen receptor (ER) binding activity of the naturally occurring (S)-enantiomer demonstrates greater affinity toward ERbeta while the (R)-enantiomer demonstrates greater...

L-DOPA is a metabolic precursor of dopamine that is capable of crossing the blood-brain barrier. It is produced from L-tyrosine by tyrosine hydroxylase and metabolized by catechol-O-methyl transferase (COMT). In the brain L-DOPA is converted to dopamine. Formulations containing L-DOPA have been used in stroke...

Davercin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains. It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria (MICs = 0.02-50 µg/ml). Davercin is non-toxic to mice...

The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. 1,5-Isoquinolinediol is an inhibitor of poly(ADP-ribose) synthetase (PARP1, IC50 = 0.39 µM). It has been used to study the role of PARP1 in both DNA repair and oxidant stress-induced cell death. This compound...

bpV(HOpic) is a bisperoxovanadium (bpV) compound that inhibits several different protein tyrosine phosphatases (PTPs), with selectivity for PTEN (IC50 = 14 nM). It also inhibits the vascular endothelial PTP, PTP-beta (IC50 = 4.9 µM), and PTP-1betaB (IC50 = 25.3 µM). At 15 µM, bpV(HOpic) has been shown to protect...

Ibudilast is an inhibitor of phosphodiesterase 4 (PDE4, IC50s = 54, 65, 239, and 166 nM for PDE4A-D, respectively). It is selective for PDE4 over PDE1, PDE7A, PDE7B, and PDE9A (IC50s = >10,000 nM for all) but does inhibit PDE3A, PDE3B, and PDE5A (IC50s = 1,600, 2,700, and 3,510 nM, respectively). Ibudilast inhibits...

Sphingosine kinase (SPHK) is an important enzyme in the sphingolipid metabolic pathway. SPHKs phosphorylate D-erythro-sphingosine to yield sphingosine-1-phosphate (S1P). To date two isoforms of SPHK, SPHK1 and SPHK2, have been identified & characterized from mammalian cells. Among them, SPHK1 has been implicated to...

MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 µM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against type II or type III PRMTs nor any additional methyltransferases...

Alfuzosin is a post-synaptic alpha1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH). It displays high-affinity with non-selectivity for the three known human alpha1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for alpha1A, alpha1B, and...