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382193 HMTase Inhibitor V, UNC0224 - CAS 1197196-48-7 - Calbiochem

382193
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₆H₄₃N₇O₂ • H₂O1197196-48-7

Products

Catalogue NumberPackaging Qty/Pack
382193-5MG Glass bottle 5 mg
Description
OverviewA quinazolinamine compound that inhibits G9a and GLP histone H3K9 methyltransferase activity (IC50 ~50 and 54 nM, respectively) by targeting the lysine binding channel, while affecting muscarinic M2 receptor and histamine H1 receptor only at much higher concentrations (by 82% and 31%, respectively, at 1 µM) and exhibiting little activity against SET7/9, SET8/PreSET7, PRMT3, JMJD2E (IC50 >40 µM), or a panel of 30 GPCR, ion channels, and transporters (<20% inhibition at 1 µM).
Catalogue Number382193
Brand Family Calbiochem®
Synonyms7-(3-Dimethylaminopropoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine, H₂O, Histone Lysine Methyltransferase Inhibitor V, UNC0224, EHMT1/GLP Inhibitor III, EHMT2/G9a Inhibitor V
References
ReferencesLiu, F., et al. 2010. J. Med. Chem. 53, 5844.
Liu, F., et al. 2009. J. Med. Chem. 52, 7950.
Product Information
CAS number1197196-48-7
FormLiquid
Hill FormulaC₂₆H₄₃N₇O₂ • H₂O
Chemical formulaC₂₆H₄₃N₇O₂ • H₂O
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% 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 Dry Ice Only
Toxicity Standard Handling
Storage ≤ -70°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

HMTase Inhibitor V, UNC0224 - CAS 1197196-48-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Liu, F., et al. 2010. J. Med. Chem. 53, 5844.
Liu, F., et al. 2009. J. Med. Chem. 52, 7950.

Technical Info

Title
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
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.

Revision26-March-2012 JSW
Synonyms7-(3-Dimethylaminopropoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine, H₂O, Histone Lysine Methyltransferase Inhibitor V, UNC0224, EHMT1/GLP Inhibitor III, EHMT2/G9a Inhibitor V
DescriptionA quinazolinamine compound that acts as a highly potent inhibitor against G9a (IC50 = 43 and 57 nM by SAHH production determination/ECSD and substrate lysine methylation detection/CLOT, respectively) and GLP (IC50 = 50 and 58 nM by ECSD and CLOT, respectively) histone H3K9 methyltransferase activity, while affecting muscarinic M2 receptor and histamine H1 receptor only at much higher concentrations (by 82% and 31%, respectively, at 1 µM) and exhibiting little activity against SET7/9, SET8/PreSET7, PRMT3, JMJD2E (IC50 >40 µM), or a panel of 30 GPCR, ion channels, and transporters (<20% inhibition at 1 µM). X-ray crystallography study reveals that UNC0224 exerts its inhibition by occupying G9a lysine binding channel via its 7-dimethylamino propoxy side chain.
FormLiquid
Intert gas (Yes/No) Packaged under inert gas
CAS number1197196-48-7
Chemical formulaC₂₆H₄₃N₇O₂ • H₂O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)
Storage ≤ -70°C
Hygroscopic
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Toxicity Standard Handling
ReferencesLiu, F., et al. 2010. J. Med. Chem. 53, 5844.
Liu, F., et al. 2009. J. Med. Chem. 52, 7950.