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.
In Vitro

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.
In Vivo

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.
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

324.3803
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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