159529
CAS Number
1255580-76-7Grade
Highly PurifiedMolecular Formula
C30H47N5O2Molecular Weight
509.73EU Commodity Code
38220090Shipping Temp
RTStorage Temp
RT/4°C2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
UNC0638
UNC0638 is a selective inhibitor of G9a and G9a-like protein (GLP), also known as EHMT1, with IC50's in the very low (<20) nM range. It also exhibits very weak activity against JMJD2E (IC50 ~4.5uM), but the selectivity for G9a and GLP is over 200-fold. UNC0638 was inactive against SUV39H1, SUV39H2, EZH2), SETD7, MLL, SMYD3, DOT1L, SETD8, PRDM1, PRMT1 and PRMT3. UNC0638 exhibits only extremely weak inhibition of DNMT1 (IC50 >100uM).
Molecular Formula
C30H47N5O2
Solubility
Soluble in DMSO purged with an inert gas, then dilute into aqueous buffer just before use. Solubility in DMSO is 20mg/ml.
Biological Activity
Inhibits G9a activity with an IC50 value of <15nM in vitro. It also inhibits GLP with an IC50 value of 19nM.
Storage and Stability
Store at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.
References
Liu, F. et al.: J. Med. Chem., 53, 5844 (2010); Kubicek, S. et al.: Mol. Cell., 25, 473 (2007); Huangfu, D et al.: Nat. Biotechnol., 26, 795 (2008); Chang, Y. et al.: Bat. Struct. Mol. Biol., 16, 312 (2009)USBio References
No references available