DS-437 | CAS#1674364-87-4 | PRMT5-PRMT7 Inhibitor |MedKoo

MedKoo Cat#: 531767 | Name: DS-437

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Description:

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

DS-437 is a dual PRMT5-PRMT7 Inhibitor.

Chemical Structure

DS-437

CAS#1674364-87-4

Theoretical Analysis

MedKoo Cat#: 531767

Name: DS-437

CAS#: 1674364-87-4

Chemical Formula: C15H23N7O4S

Exact Mass: 397.1532

Molecular Weight: 397.45

Elemental Analysis: C, 45.33; H, 5.83; N, 24.67; O, 16.10; S, 8.07

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 700.00	2 Weeks
50mg	USD 1,250.00	2 Weeks

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Related CAS #

No Data

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/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	125.0	314.50

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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.