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476496 Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem

Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem: Malzeme Güvenlik Bilgi Formu (MSDS) veya SDS, Analiz Sertifikası (COA) ve Kalite Uygunluk Sertifikası (COQ), dosyalar, broşürler ve diğer dokümanlar.

Synonyms: 7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine

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476496
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Overview

Key Spec Table

Empirical Formula
C₂₇H₄₅N₇O₃

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476496-5MG
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      Description
      OverviewA 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 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 (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.
      Catalogue Number476496
      Brand Family Calbiochem®
      Synonyms7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
      References
      ReferencesLiu, F., et al. 2010. J. Med. Chem. 53, 5844.
      Product Information
      FormLight tan solid
      Hill FormulaC₂₇H₄₅N₇O₃
      Chemical formulaC₂₇H₄₅N₇O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity>98% by HPLC
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      476496-5MG 04055977183856