UNC0224

UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E[1][2].

Product Specifications

CAS Number

[1197196-48-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/UNC0224.html

Purity

98.85

Solubility

DMSO : 16.67 mg/mL (ultrasonic)

Smiles

CN1CCC(NC2=C3C=C(OC)C(OCCCN(C)C)=CC3=NC(N4CCN(C)CCC4)=N2)CC1

Molecular Formula

C26H43N7O2

Molecular Weight

485.67

Precautions

H302, H315, H319, H335

References & Citations

[1]Liu F, et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem. 2009 Dec 24;52 (24) :7950-3.|[2]Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53 (15) :5844-57.