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9(12):2126-39
and the apparent Ki is 2
Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1
PIK-III is at least 100-fold-selective for VPS34 over related lipid kinases such as PI3K and the protein kinase mTOR
PubMed Central PMCID: PMC3820652
KDM5-C49 - JARID1 Histone Demethylases Inhibitor. CAS# 1596348-16-1 319 9(12):2126-39KDM5 C49, CAS No. 1596348 16 1, is a potent and selective inhibitor of Jumonji AT Rich Interactive Domain 1 (JARID1) histone demethylases. It has IC50 ~40 nM, 160 nM and 100 nM for KDM5A, KDM5B and KDM5C respectively. It has >100 fold selectivity over KDM4 and KDM6 etc. KDM5 C49 occupies the aKG binding site. The highly polar carboxylate group of KDM5 C49 restricts its cellular permeability, so it has IC50 >1 M for inhibiting demthylation of H3K4 in
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