1. Epigenetics
  2. Histone Methyltransferase
  3. DS-437

DS-437 

Cat. No.: HY-124131
Handling Instructions

DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.

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

DS-437 Chemical Structure

DS-437 Chemical Structure

CAS No. : 1674364-87-4

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Description

DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3[1][2].

In Vitro

DS-437 was able to inhibit methylation of an H4[1–24] peptide by the PRMT5–MEP50 complex under balanced conditions (cofactor and substrate concentrations set at their respective Km values) in a dose-dependent manner with an IC50 of 5.9 ± 1.4 μM[1].
DS-437 increased total CD8+ and CD8+ PD-1+ T cells[2].

In Vivo

DS-437 (10 mg/kg; i.p.; 5 times a week) has some beneficial effects on inhibiting tumor growth. The combination of DS-437 and the anti-p185erbB2/neu antibody 4D5 had even more dramatic effects[1].

Animal Model: Six to Ten weeks old female Balb/c mice (bearing  CT26Her2 tumor cells)[1]
Dosage: 10 mg/kg
Administration: i.p.; 5 times a week
Result: Had some beneficial effects on inhibiting tumor growth.
Molecular Weight

397.45

Formula

C₁₅H₂₃N₇O₄S

CAS No.

1674364-87-4

SMILES

O[[email protected]@H]([[email protected]]([[email protected]](N1C=NC2=C(N=CN=C21)N)O3)O)[[email protected]]3CSCCNC(NCC)=O

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

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Keywords:

DS-437DS437DS 437Histone MethyltransferaseargininemethyltransferasesPRMT5-MEP50complextumor,?TcellsInhibitorinhibitorinhibit

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DS-437
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