MilliporeSigma™ Calbiochem™ Protein Lysine Methyltransferase Inhibitor, UNC0321

A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC_{50 = 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}

Manufacturer:  MilliporeSigma™ 4764965MG

Catalog No. 47-649-65MG

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 K_i = 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.

Specifications

• Description: >98% by HPLC
• Storage Requirements: Protect from Light
• Molecular Formula: C₂₇H₄₅N₇O₃

• Format: Light tan solid
• Quantity: 5mg
• Solubility: DMSO