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KDM5A-IN-50

Chemical Structure : KDM5A-IN-50

CAS No.: 1905481-36-8

KDM5A-IN-50 (pan KDM5 inhibitor)

Catalog No.: PC-62835Not For Human Use, Lab Use Only.

KDM5A-IN-50 is a potent, selective, and orally bioavailable pan KDM5 enzyme inhibitor with biochemical IC50 of 45/56/55 nM for KDM5A/KDM5B/KDM5C respectively.

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

Biological Activity

KDM5A-IN-50 is a potent, selective, and orally bioavailable pan KDM5 enzyme inhibitor with biochemical IC50 of 45/56/55 nM for KDM5A/KDM5B/KDM5C respectively.
KDM5A-IN-50 significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 6A, 7B).
KDM5A-IN-50 inhibits H3K4Me3 level in PC9 cells with EC50 of 960 nM; has promising in vivo PK profiles.

Physicochemical Properties

M.Wt 290.367
Formula C15H22N4O2
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

10 mM in DMSO

Chemical Name/SMILES

(R)-N-(1-(5-isopropyl-1H-pyrazole-3-carbonyl)pyrrolidin-3-yl)cyclopropanecarboxamide

References

1. Liang J, et al. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981.

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