KDM5-IN-1 是一种有效的特异性 KDM5 抑制剂，IC50 为 15.1 nM。

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

KDM5-IN-1 is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 potently inhibits KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively)[1].

KDM5-IN-1(50 mg/kg; oral) shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50 in vivo[1].

1628210-26-3

C17H20N6O

324.38

DMSO:30 mg/mL (92.48 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years