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KDM5-IN-48

Chemical Structure : KDM5-IN-48

CAS No.: 1628210-26-3

KDM5-IN-48

Catalog No.: PC-42149Not For Human Use, Lab Use Only.

KDM5-IN-48 is 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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

KDM5-IN-48 is 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.
KDM5-IN-48 displays significantly less potent against other KDM enzymes (KDM4C IC50=1.9 uM).
KDM5-IN-48 increases H3K4Me3 level in PC9 cells with EC50 of 0.34 uM.
KDM5-IN-48 possesses suitable physiochemical properties and displays excellent PK profile in mice.

Physicochemical Properties

M.Wt 324.3803
Formula C17H20N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

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

References

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

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