CARM1 INHIBITOR 1PC X 10MG

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

Molecular Weight: 555.26. Empirical Formula: C₂₆H₂₁Br₂NO₃. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.