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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.

Synonyme(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

Formule empirique (notation de Hill):
C26H21Br2NO3
Numéro CAS:
1020399-49-8
Poids moléculaire :
555.26
Numéro MDL:
MFCD23115307
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.28

Niveau de qualité

100

Pureté

≥95% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

orange

Solubilité

DMSO: 50 mg/mL

Conditions d'expédition

ambient

Température de stockage

2-8°C

Chaîne SMILES 

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

Description générale

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).

Actions biochimiques/physiologiques

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,

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Consulter la Bibliothèque de documents

Macheng Lu et al.
Oncology reports, 51(1) (2023-11-24)
Ribosome production factor 2 homolog (RPF2) plays an important role in the life processes of ribosomal biogenesis; however, the function and mechanism of RPF2 in tumors are unclear. The present study demonstrated that RPF2 expression is involved in chemoresistance in
Ricardo de Matos Simoes et al.
Nature cancer, 4(5), 754-773 (2023-05-27)
Clinical progress in multiple myeloma (MM), an incurable plasma cell (PC) neoplasia, has been driven by therapies that have limited applications beyond MM/PC neoplasias and do not target specific oncogenic mutations in MM. Instead, these agents target pathways critical for
Yiming Cheng et al.
Molecular therapy. Nucleic acids, 34, 102063-102063 (2023-11-29)
Ferroptosis is an iron-catalyzed form of regulated cell death that results from the accumulation of lipid peroxidation products and reactive oxygen species to a lethal content. However, the transcriptional regulation of ferroptosis is not well understood. Sorafenib, a standard drug
Yugo Ishino et al.
Developmental neurobiology, 82(3), 245-260 (2022-02-28)
Protein arginine methylation has been recognized as one of key posttranslational modifications for refined protein functions, mediated by protein arginine methyltransferases (Prmts). Coactivator-associated arginine methyltransferase (Carm1, also known as Prmt4) participates in various cellular events, such as cell survival, proliferation

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