476496 Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem

Overview

Replacement Information

Key Specifications 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
      Applications
      Biological Information
      Purity>98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem Certificates of Analysis

      TitleLot Number
      476496

      References

      Reference overview
      Liu, F., et al. 2010. J. Med. Chem. 53, 5844.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision21-November-2014 JSW
      Synonyms7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
      DescriptionA 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 Ki 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.
      FormLight tan solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₄₅N₇O₃
      Structure formulaStructure formula
      Purity>98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      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.
      Toxicity Standard Handling
      ReferencesLiu, F., et al. 2010. J. Med. Chem. 53, 5844.