1. Epigenetics
  2. Histone Methyltransferase
  3. MS049 dihydrochloride

MS049 dihydrochloride 

Cat. No.: HY-100360A
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MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and do not affect the growth of HEK293 cells.

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MS049 dihydrochloride Chemical Structure

MS049 dihydrochloride Chemical Structure

CAS No. : 2095432-59-8

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Description

MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and do not affect the growth of HEK293 cells[1].

In Vitro

MS049 dihydrochloride (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM)[1].
MS049 dihydrochloride (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells[1].
MS049 dihydrochloride is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets[1].

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 20 hours
Result: Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM).

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells.
Molecular Weight

321.29

Formula

C₁₅H₂₆Cl₂N₂O

CAS No.

2095432-59-8

SMILES

CNCCN1CCC(OCC2=CC=CC=C2)CC1.[H]Cl.[H]Cl

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

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Keywords:

MS049MS 049MS-049Histone MethyltransferaseepigeneticmodifiersselectiveargininedimethylationtoxicH4R3me2aHEK293cellsInhibitorinhibitorinhibit

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MS049 dihydrochloride
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