KDM5-IN-48 ( KDM5-IN-48; KDM5 IN 48; KDM5IN48; KDM5 inhibitor-48; KDM5 inhibitor 48 )

Catalog No. M12424 CAS No. 1628210-26-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

KDM5-IN-48
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
Synonyms

KDM5-IN-48; KDM5 IN 48; KDM5IN48; KDM5 inhibitor-48; KDM5 inhibitor 48
Pathway

Chromatin/Epigenetic
Target

Histone Demethylase
Recptor

Histone Demethylase
Research Area

——
Indication

——

CAS Number

1628210-26-3
Formula Weight

324.38
Molecular Formula

C17H20N6O
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 30 mg/mL
SMILES

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

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

1. Liang J, et al. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41.

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