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476496 Protein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Replacement Information

Key Specifications Table

Empirical Formula
C₂₇H₄₅N₇O₃

Products

Catalog NumberPackaging Qty/Pack
476496-5MG Glass bottle 5 mg
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
Global Trade Item Number
Catalog Number GTIN
476496-5MG 04055977183856

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 Protect from light
-20°C
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.