Products
BRL-50481
BRL-50481 is a potent and selective inhibitor of phosphodiesterase-7 (PDE7), Ki=180 nM. Induces apoptosis in chronic lymphocytic leukemia cells which express PDE7B. Increases mineralization in osteoblasts differentiated from hMSC. Cell…
C-646
A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. Demonstrates 86% inhibition against p300 at 10 nM. Less…
Decitabine
Cytosine analog, that when incorporated into DNA, acts as a suicide substrate for DNA methyltransferase. Inhibits DNA methyltransferase and results in DNA hypomethylation and activation of silent genes. Chemotherapeutic agent;…
DMXAA
Intratumoral administration of DMXAA resulted in tumor regression and complete rejection in mouse xenografts. Tumor regression induced by DMXAA results from a cascade of cellular events which include disruption of…
EX-527
EX-527 is a cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM in vivo, 38nM in vitro) that does not inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members…
Garcinol
Garcinol is an inhibitor of the histone acetyltransferases (HATs) p300 and PCAF with IC50 of 7 and 5 uM, respectively. It also inhibits the HAT GCN5 in Cryptococcus neoformans, inducing…
H-151
H-151 covalently binds to Cys91 of STING preventing activation via blockade of palmitoylation and clustering STING. H-151 blocks STING induced expression of pro-inflammatory cytokines and reduces inflammation in models of…
IBMX
IBMX is a widely-used non-specific inhibitor of cyclic AMP and cyclic GMP phosphodiesterases (PDEs) with IC50s from 7 to 50 µM for PDE1-5, PDE7, and PDE11. PDE8A, PDE8B, and PDE9…
IOX1
Inhibits the JMJD family of 2-oxoglutarate-dependent histone demethylases. IC50 = 0.12, 0.07, 0.2, 0.3, 0.6, and 1 μM for JMJD3, JMJD1A, JMJD2A, JMJD2E, JMJD2C and UTX respectively. Is a broad…
Phenylbutyrate, Na Salt
Histone deacetylase inhibitor that displays anticancer activity. Inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. Also inhibits protein isoprenylation, depletes plasma glutamine, increases production of fetal…
Piceatannol
Activator of human deacetylase SIRT1. Anti-inflammatory, immunomodulatory and antiproliferative agent that inhibits p56lck and syk protein tyrosine kinases and inhibits TNF-induced NF-kB activation and gene expression. Piceatannol is a resveratrol…
Resveratrol
Potent SIRT1 activator and a phytoestrogen with antitumor, antioxidant, antiplatelet, anti-inflammatory and antifungal effects. Inhibits cytochrome P450 1A1 (IC50 = 23 uM) and displays mixed agonist/antagonist actions at ERalpha and…
Sirtinol
Cell-permeable, selective sirtuin deacetylase inhibitor (IC50 values are 38, 68 and 131 uM for SIRT2, Sir2p and SIRT1 respectively) that has no effect on HDAC1 activity. Significantly decreases growth and…
Sodium Valproate
An anticonvulsant used in the treatment of epilepsy, anorexia nervosa, panic attack, anxiety disorder, post traumatic stress disorder, migraine and bipolar disorder. Valproate is also a histone deacetylase inhibitor (IC50…