2095432-59-8

2095432-59-8 structure

Name: MS049 dihydrochloride
Chemical Name: MS049 dihydrochloride
CAS Number: 2095432-59-8
Molecular Formula: C₁₅H₂₆Cl₂N₂O
Molecular Weight: 321.29
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2020-06-01 16:26:50
Modify Date: 2024-01-10 15:18:18
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].

Name	MS049 dihydrochloride

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Methyltransferase
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.
References	[1]. Shen Y et al. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Oct 13;59(19):9124-9139.

Molecular Formula	C₁₅H₂₆Cl₂N₂O
Molecular Weight	321.29

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