Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem (C15-1303-852)

General description

A cell-permeable quinazoline analog that potently and selectively inhibits PKMT G9a with IC₅₀s equal to 6 µM and 9 µM in two biochemical assays (CLOT and ECSD respectively), and a Morrison K_i of 63 pM, which is about 250-fold more potent compared with a close analog BIX01294 (Cat. No. 382190). Also inhibited GLP with reduced potency (15 µM in an ECSD enzymatic assay). It was found to be inactive (IC₅₀>40 µM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3 in the ECSD assays as well as JMJD2E with >1000-fold selectivity.

A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC₅₀ = 6 nM and 9 nM 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 (15 nM) and is found to be inactive (IC₅₀ >40 µM) 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 = 11,000 nM) in MDA-MB-231 cells, in comparison to BIX01294 (IC₅₀ = 500 nM).

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Liu, F., et al. 2010. J. Med. Chem.53, 5844.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 515.69. Empirical Formula: C₂₇H₄₅N₇O₃. Assay: >. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: light tan. solubility: DMSO: 100 . mg/mL. shipped in: wet ice. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.