UNC0638

Catalog #

27222

$195 *

Size: 5 mg

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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).

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Product Info

Storage and Usage

Citations

Purity

≥98% by HPLC

Format

A crystalline solid.

Formula

C₃₀H₄₇N₅O₂

509.7 Da

Solubility

Soluble in DMSO purged with an inert gas, then dilute into aqueous buffer just before use. Solubility in DMSO is 20 mg/ml.

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 Registry #

1255580-76-7

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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