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217531 CARM1 Inhibitor - CAS 1020399-49-8 - Calbiochem

217531
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1020399-49-8C₂₆H₂₁Br₂NO₃

Products

Catalogue NumberPackaging Qty/Pack
217531-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50 = 7.1 µM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100 µM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50 >100 µM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor).
Catalogue Number217531
Brand Family Calbiochem®
SynonymsPRMT Inhibitor V, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one
References
ReferencesCheng, D., et al. 2011. J. Med. Chem. 54, 4928.
Product Information
CAS number1020399-49-8
FormOrange solid
Hill FormulaC₂₆H₂₁Br₂NO₃
Chemical formulaC₂₆H₂₁Br₂NO₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPRMT4
Primary Target IC<sub>50</sub>CARM1-mediated methylation over PRMT1 and SET7 (IC₅₀ = 7.1, 63 and 943 µM,
Secondary targetSET7
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°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
Catalogue Number GTIN
217531-10MG 04055977219388

Documentation

CARM1 Inhibitor - CAS 1020399-49-8 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

CARM1 Inhibitor - CAS 1020399-49-8 - Calbiochem Certificates of Analysis

TitleLot Number
217531

References

Reference overview
Cheng, D., et al. 2011. J. Med. Chem. 54, 4928.
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.

Revision18-July-2012 JSW
SynonymsPRMT Inhibitor V, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one
DescriptionA cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50 = 7.1 µM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100 µM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50 >100 µM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor).
FormOrange solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1020399-49-8
Chemical formulaC₂₆H₂₁Br₂NO₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°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
ReferencesCheng, D., et al. 2011. J. Med. Chem. 54, 4928.