KDM5-IN-48

Research use only, not for human use.

A potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively.

A potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively; displays significantly less potent against other KDM enzymes (KDM4C IC50=1.9 uM); increases H3K4Me3 level in PC9 cells with EC50 of 0.34 uM; possesses suitable physiochemical properties and displays excellent PK profile in mice.

KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It 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 still displays more than 100-fold selectivity for KDM4C vs. KDM5A.

When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo.

KDM5-IN-48 | KDM5 IN 48 | KDM5IN48 | KDM5 inhibitor-48 | KDM5 inhibitor 48

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

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1628210-26-3

324.3803

C17H20N6O

>98% (HPLC)

DMSO: ≥ 30 mg/mL

N#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O

Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 5-[1-(1,1-dimethylethyl)-1H-pyrazol-4-yl]-4,7-dihydro-6-(1-methylethyl)-7-oxo-

(-20℃)

With Ice Pack

≥ 2 years