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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.

Sinónimos:

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

Fórmula empírica (notación de Hill):
C26H21Br2NO3
Número de CAS:
1020399-49-8
Peso molecular:
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

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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