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159529 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine CAS: 1255580-76-7

Specifications
References
CAS Number
1255580-76-7
Grade
Highly Purified
Molecular Formula
C30H47N5O2
Molecular Weight
509.73
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
RT/4°C
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).

Alternate Name
UNC0638
CAS Number
1255580-76-7
Molecular Formula
C30H47N5O2
Molecular Weight
509.73
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.
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
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