1674364-87-4
1674364-87-4 structure
- Name: DS-437
- Chemical Name: DS-437
- CAS Number: 1674364-87-4
- Molecular Formula: C15H23N7O4S
- Molecular Weight: 397.453
- Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
- Create Date: 2020-01-14 11:00:12
- Modify Date: 2025-08-25 17:28:24
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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.
| Name | DS-437 |
|---|---|
| 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]- |
| 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. |
| 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 |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | Missing Phrase - N15.00950417 |
| RIDADR | UN 2811 6.1 / PGIII |