217531

CARM1 Inhibitor

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

• 別名: 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
• 実験式（ヒル表記法）: C₂₆H₂₁Br₂NO₃
• CAS番号: 1020399-49-8
• 分子量: 555.26
• MDL番号: MFCD23115307
• UNSPSCコード: 12352200
• NACRES: NA.28

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: 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
• InChI Key: KNMFTTWVELIVCC-CLVAPQHMSA-N

詳細

詳細

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).

生物化学的／生理学的作用

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,

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable