476496

UNC0321

>98% (HPLC), solid, protein lysine methyltransferase inhibitor, Calbiochem^®

• Synonym(e): Protein Lysine Methyltransferase Inhibitor, UNC0321, 7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
• Empirische Formel (Hill-System): C₂₇H₄₅N₇O₃
• Molekulargewicht: 515.69
• UNSPSC-Code: 12352202
• NACRES: NA.77

Eigenschaften

• product name: Protein Lysine Methyltransferase Inhibitor, UNC0321,
• Assay: >98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light tan
• Löslichkeit: DMSO: 100 mg/mL
• Versandbedingung: wet ice
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable