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

DS-437 

Cat. No.: HY-124131 Purity: 99.61%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
25 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 700 In-stock
Estimated Time of Arrival: December 31
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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (314.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5160 mL 12.5802 mL 25.1604 mL
5 mM 0.5032 mL 2.5160 mL 5.0321 mL
10 mM 0.2516 mL 1.2580 mL 2.5160 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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Product Name:
DS-437
Cat. No.:
HY-124131
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