KDM5A-IN-1

KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) [1].

Product Specifications

CAS Number

[1905481-36-8]

UNSPSC

12352005

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/KDM5A-IN-1.html

Purity

99.95

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1CC1)N[C@@H]2CCN(C(C3=CC(C(C)C)=NN3)=O)C2

Molecular Formula

C15H22N4O2

Molecular Weight

290.37

References & Citations

[1]Liang J, et al. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27 (13) :2974-2981.