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1674364-87-4

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1674364-87-4 Structure

1674364-87-4 Structure
IdentificationBack Directory
[Name]

DS-437
[CAS]

1674364-87-4
[Synonyms]

DS-437
DS-437 (DS437
DS-437 >=98% (HPLC)
Adenosine, 5'-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5'-thio-
[Molecular Formula]

C15H23N7O4S
[MDL Number]

MFCD32661891
[MOL File]

1674364-87-4.mol
[Molecular Weight]

397.45
Chemical PropertiesBack Directory
[storage temp. ]

2-8°C
[solubility ]

DMSO:125.0(Max Conc. mg/mL);314.5(Max Conc. mM)
[form ]

powder
[color ]

white to beige
Safety DataBack Directory
[Symbol(GHS) ]


GHS06
[Signal word ]

Danger
[Hazard statements ]

H301
[Precautionary statements ]

P301+P330+P331+P310
[RIDADR ]

UN 2811 6.1 / PGIII
Hazard InformationBack Directory
[Description]

DS-437 is a dual inhibitor of protein arginine methyltransferase 5 (PRMT5) and PRMT7 (IC50s = 5.9 and 6 μM, respectively). It is selective for PRMT5 and PRMT7 over a panel of 29 additional protein, DNA, and RNA methyltransferases at 50 μM, but also inhibits DNMT3A and DNMT3B (IC50s = 52 and 62 μM, respectively). DS-437 (2.5 and 10 μM) inhibits symmetrical arginine dimethylation of FOXP3 in HEK293T cells, as well as symmetrical arginine dimethylation of p60 and the ribonucleoproteins SmD1/D3 and SmB/B’ in MDA-MB-231 cells in a concentration-dependent manner. It inhibits the ability of regulatory T cells (Tregs) to suppress effector T cell (Teff) proliferation in vitro in human and murine Treg suppression assays. DS-437 (10 mg/kg five times per week) reduces tumor growth in a CT26Her2 murine colon cancer model when administered in combination with the anti-p185erbB2/neu antibody 4D5.
[Uses]

DS-437 has been used as an inhibitor of protein arginine methyltransferase 5 (PRMT5) to study its effect on forkhead box P3 (FOXP3) methylation and regulatory T cells (Tregs) function in 293T cells.
[Biochem/physiol Actions]

DS-437 is an analog of S-adenosyl methionine (SAM ), which inhibits protein arginine methyltransferases PRMT5 and PRMT7 (IC50 5.9 and 6 μM) with little interaction against a panel of 30 other human methyltransferases.
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