DS-437

Modify Date: 2024-01-09 20:06:05

DS-437 Structure
DS-437 structure
Common Name DS-437
CAS Number 1674364-87-4 Molecular Weight 397.453
Density 1.7±0.1 g/cm3 Boiling Point N/A
Molecular Formula C15H23N7O4S Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS06
GHS06
Signal Word Danger

 Use of DS-437


DS-437 is a potent, selective, dual inhibitor of PRMT5 and PRMT7 with IC50 of 6.0 uM for both, DS-437 is inactive against 29 other human protein-, DNA-, and RNA-methyltransferases; inhibits methylation of full-length histone 4 by PRMT5-MEP50 with an IC50 of 37 ± 1.2 μM in a biochemical assay; inhibits symmetrical dimethylation of PRMT5 substrates in cells.

 Names

Name DS-437
Synonym More Synonyms

 DS-437 Biological Activity

Description DS-437 is a potent, selective, dual inhibitor of PRMT5 and PRMT7 with IC50 of 6.0 uM for both, DS-437 is inactive against 29 other human protein-, DNA-, and RNA-methyltransferases; inhibits methylation of full-length histone 4 by PRMT5-MEP50 with an IC50 of 37 ± 1.2 μM in a biochemical assay; inhibits symmetrical dimethylation of PRMT5 substrates in cells.
Related Catalog
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.
References

[1]. Smil D, et al. Discovery of a Dual PRMT5-PRMT7 Inhibitor.ACS Med Chem Lett. 2015 Mar 2;6(4):408-12.

[2]. Nagai Y, et al. PRMT5 Associates With the FOXP3 Homomer and When Disabled Enhances Targetedp185erbB2/neu Tumor Immunotherapy.Front Immunol. 2019 Feb 8;10:174.

 Chemical & Physical Properties

Density 1.7±0.1 g/cm3
Molecular Formula C15H23N7O4S
Molecular Weight 397.453
Exact Mass 397.153229
LogP 0.16
Index of Refraction 1.776
Storage condition 2-8°C

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements Missing Phrase - N15.00950417
RIDADR UN 2811 6.1 / PGIII

 Synonyms

9-[(2ξ)-5-S-{2-[(Ethylcarbamoyl)amino]ethyl}-5-thio-β-D-threo-pentofuranosyl]-9H-purin-6-amine
DS-437
5'-S-[2-[[(Ethylamino)carbonyl]amino]ethyl]-5'-thio-adenosine
9H-Purin-6-amine, 9-[(2ξ)-5-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5-thio-β-D-threo-pentofuranosyl]-
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