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 )
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KDM5A-IN-1
CAS number：1905481-36-8(DMSO) molecular formula：C15H22N4O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1905481-36-8(DMSO) | molecular formula | C15H22N4O2 |
| molecular weight | 290.36 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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