A dual inhibitor of PRMT5 and PRMT7 (IC50s = 5.9 and 6 μM

DS-437 – 10 mg

Brand:
Cayman
CAS:
1674364-87-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

DS-437 is a dual inhibitor of protein arginine methyltransferase 5 (PRMT5) and PRMT7 (IC50s = 5.9 and 6 μM, respectively).{53117} 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.{53117,53118} 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.{53118} 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.  

 

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SKU: 29476 - 10 mg Category:

Description

A dual inhibitor of PRMT5 and PRMT7 (IC50s = 5.9 and 6 μM, respectively); 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); inhibits symmetrical arginine dimethylation of FOXP3 in HEK293T cells at 2.5 and 10 μM; inhibits the ability of Tregs to suppress Teff proliferation in vitro in human and murine Treg suppression assays; reduces tumor growth in a CT26Her2 murine colon cancer model when administered at 10 mg/kg five times per week in combination with the anti-p185erbB2/neu antibody 4D5

Formal name: 5′-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5′-thio-adenosine

Synonyms: 

Molecular weight: 397.5

CAS: 1674364-87-4

Purity: ≥98%

Formulation: A solid

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