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217531

Sigma-Aldrich

CARM1 Inhibitor

The CARM1 Inhibitor controls the biological activity of CARM1. This small molecule/inhibitor is primarily used for Cell Structure applications.

Synonym(s):

CARM1 Inhibitor, 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, PRMT 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, PRMT Inhibitor V

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About This Item

Empirical Formula (Hill Notation):
C26H21Br2NO3
CAS Number:
1020399-49-8
Molecular Weight:
555.26
MDL number:
MFCD23115307
UNSPSC Code:
12352200
NACRES:
NA.28

Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

O=C(/C(CN(CC1=CC=CC=C1)C/2)=C/C3=CC=C(O)C(Br)=C3)C2=C\C4=CC(Br)=C(O)C=C4

General description

A 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).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PRMT4
Reversible: yes
Secondary Target
SET7
Target IC50: CARM1-mediated methylation over PRMT1 and SET7 (IC₅₀ = 7.1, 63 and 943 µM,

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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