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Biological Activity: UNC0638 inhibits G9a activity with an IC50 value of <15 nM in vitro. It also inhibits GLP with an IC50 value of 19 nM.
CAS Number: 1255580-76-7
Description: 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 ~4.5 µM), 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 >100 µM).
Format: A crystalline solid
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO purged with an inert gas, then dilute into aqueous buffer justbefore use. Solubility in DMSO is 20 mg/ml.
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Biosafety Level: Not applicable (BSL-1)
References: 1. Tachibana, M., et al., Genes Dev. 2002; 16:1779-1791.
2. Wagschal, A., et al., Mol. Cell. Biol. 2008; 28(3):1104-1113.
3. Thomas, L.R., et al., J. Immunol. 2008; 181:485-493.
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