1. Epigenetics
  2. Histone Methyltransferase
  3. MS117

MS117 

Cat. No.: HY-133740
Handling Instructions

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.

For research use only. We do not sell to patients.

MS117 Chemical Structure

MS117 Chemical Structure

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Description

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM[1].

IC50 & Target

IC50: 18 nM (PRMT6), 100 nM (PRMT1), 110 nM (PRMT8), 3 μM (PRMT3), 4 μM (PRMT4)[1].

In Vitro

MS117 (Compound 4) inhibits the PRMT6 methyltransferase activity in a time-dependent manner[1].
MS117 (Compound 4) shows moderate selectivity (6-fold) for PRMT6 over PRMT1 (IC50 = 0.1 ± 0.025 µM) and PRMT8 (IC50 = 0.11 ± 0.01 µM) [1].

Molecular Weight

298.38

Formula

C₁₇H₂₂N₄O

SMILES

NCCN(C)CC1=CNC=C1C2=CC=CC(NC(C=C)=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MS117MS 117MS-117Histone MethyltransferaseInhibitorinhibitorinhibit

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MS117
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