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MilliporeSigma™ Calbiochem™ Protein Lysine Methyltransferase Inhibitor, UNC0321

Catalog No. 4764965MG Shop All MilliporeSigma Products
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Description

A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC50 = 6nM and 9nM in two biochemical assays for CLOT and ECSD, respectively, and Ki = 63 pM, which is approximately 250-fold more potent than a closely-related analog, BIX0129

A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC50 = 6nM and 9nM in two biochemical assays for CLOT and ECSD, respectively, and Ki = 63 pM, which is approximately 250-fold more potent than a closely-related analog, BIX01294 (Cat. No. 382190)). It inhibits GLP with reduced potency (15nM) and is found to be inactive (IC50 > 40μM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3, as well as JMJD2E (> 1000-fold selectivity) in ECSD enzymatic assays. It also inhibits H3K9me2 accumulation (IC50 = 11,000nM) in MDA-MB-231 cells, in comparison to BIX01294 (IC50 = 500nM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
TRUSTED_SUSTAINABILITY

Specifications

Color Light Tan
Description >98% by HPLC
Molecular Formula C27H45N7O3
Solubility DMSO
Content And Storage Protect from light
Form Solid
Quantity 5 mg
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