KDM5A-IN-1

小分子

KDM5A-IN-1

K655696-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

KDM5A-IN-1 is a potent, orally bioavailable pan- histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 45 nM, 56 nM and 55 nM for KDM5A , KDM5B and KDM5C , respectively, and with an EC 50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) In Vivo KDM5A-IN-1 (Compound 50, 5 mg/kg; oral administration; female CD-1 mice) treatment shows moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%), with t 1/2 of 0.4 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice Dosage: 5 mg/kg Administration: Oral administration (Pharmacokinetic study) Result: Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%). IC50& Target:IC50: 45 nM ( KDM5A ), 56 nM ( KDM5B ) and 55 nM ( KDM5C )

KDM5A-IN-1 是一种口服生物活性泛组蛋白赖氨酸去甲基化酶 5 (KDM5) 抑制剂，对 KDM5A、KDM5B 和 KDM5C 的 IC 50 s 分别为 45 nM、56 nM 和 55 nM，对 PC9 H3K4Me3 的 EC 50 值为 960 nM。KDM5A-IN-1 对 PC9 H3K4Me3

1905481-36-8(DMSO)

C15H22N4O2

290.36 g/mol

CC(C)C1=CC(=NN1)C(=O)N2CCC(C2)NC(=O)C3CC3