DS-437
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531767

CAS#: 1674364-87-4

Description: DS-437 is a dual PRMT5-PRMT7 Inhibitor.

Chemical Structure

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DS-437
CAS# 1674364-87-4
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531767
Name: DS-437
CAS#: 1674364-87-4
Chemical Formula: C15H23N7O4S
Exact Mass: 397.15
Molecular Weight: 397.454
Elemental Analysis: C, 45.33; H, 5.83; N, 24.67; O, 16.10; S, 8.07

Price and Availability

Size Price Availability Quantity
5mg USD 275 2 weeks
25mg USD 750 2 weeks
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Synonym: DS-437; DS 437; DS437.

IUPAC/Chemical Name: 1-(2-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)ethyl)-3-ethylurea

InChi Key: CACMCLIHCDTJHL-IDTAVKCVSA-N

InChi Code: InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1

SMILES Code: O=C(NCCSC[C@H]1O[C@@H](N2C=NC3=C(N=CN=C23)N)[C@@H]([C@@H]1O)O)NCC

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM).
In vitro activity: Using available structures of PRMT5, this study designed DS-437, a PRMT5 inhibitor with an IC50 value of 6 μM against both PRMT5 and PRMT7 that is inactive against 29 other human protein-, DNA-, and RNA-methyltransferases and inhibits symmetrical dimethylation of PRMT5 substrates in cells. Reference: ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. https://pubmed.ncbi.nlm.nih.gov/25893041/
In vivo activity: By contrast, a PRMT7 inhibitor (DS-437) reduced mNaV1.9 currents in Scn11a+/+ mice. DS-437 significantly inhibited the action potential frequency of DRG neurons and relieved pain hypersensitivity in Scn11aA796G/A796G mice. Reference: Pain. 2022 Apr 1;163(4):753-764. https://pubmed.ncbi.nlm.nih.gov/34326297/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 125.0 314.50

Preparing Stock Solutions

The following data is based on the product molecular weight 397.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. doi: 10.1021/ml500467h. PMID: 25893041; PMCID: PMC4394339. 2. Ma T, Li L, Chen R, Yang L, Sun H, Du S, Xu X, Cao Z, Zhang X, Zhang L, Shi X, Liu JY. Protein arginine methyltransferase 7 modulates neuronal excitability by interacting with NaV1.9. Pain. 2022 Apr 1;163(4):753-764. doi: 10.1097/j.pain.0000000000002421. PMID: 34326297; PMCID: PMC8929296. 3. Nagai Y, Ji MQ, Zhu F, Xiao Y, Tanaka Y, Kambayashi T, Fujimoto S, Goldberg MM, Zhang H, Li B, Ohtani T, Greene MI. PRMT5 Associates With the FOXP3 Homomer and When Disabled Enhances Targeted p185erbB2/neu Tumor Immunotherapy. Front Immunol. 2019 Feb 8;10:174. doi: 10.3389/fimmu.2019.00174. PMID: 30800128; PMCID: PMC6375878.
In vitro protocol: 1. Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. doi: 10.1021/ml500467h. PMID: 25893041; PMCID: PMC4394339.
In vivo protocol: 1. Ma T, Li L, Chen R, Yang L, Sun H, Du S, Xu X, Cao Z, Zhang X, Zhang L, Shi X, Liu JY. Protein arginine methyltransferase 7 modulates neuronal excitability by interacting with NaV1.9. Pain. 2022 Apr 1;163(4):753-764. doi: 10.1097/j.pain.0000000000002421. PMID: 34326297; PMCID: PMC8929296. 2. Nagai Y, Ji MQ, Zhu F, Xiao Y, Tanaka Y, Kambayashi T, Fujimoto S, Goldberg MM, Zhang H, Li B, Ohtani T, Greene MI. PRMT5 Associates With the FOXP3 Homomer and When Disabled Enhances Targeted p185erbB2/neu Tumor Immunotherapy. Front Immunol. 2019 Feb 8;10:174. doi: 10.3389/fimmu.2019.00174. PMID: 30800128; PMCID: PMC6375878.

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1: Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett. 2015 Mar 2;6(4):408-12. doi: 10.1021/ml500467h. PubMed PMID: 25893041; PubMed Central PMCID: PMC4394339.