For research use only. Not for therapeutic Use.
DS-437(CAT:I006549) is a dual PRMT5/7 inhibitor with IC₅₀ ≈ 6 μM, showing strong selectivity for PRMT5/7 over 29 other human methyltransferases. It acts as a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5 and also weakly inhibits DNMT3A (IC₅₀ = 52 μM) and DNMT3B (IC₅₀ = 62 μM). DS-437 effectively blocks methylation of FOXP3 and suppresses H4 peptide methylation by the PRMT5–MEP50 complex (IC₅₀ = 5.9 ± 1.4 μM). In vivo, DS-437 (10 mg/kg, i.p.) exhibits antitumor activity, which is further enhanced when combined with the anti-p185erbB2/neu antibody 4D5, supporting its potential in epigenetic cancer therapy.
| CAS Number | 1674364-87-4 |
| Synonyms | 1-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylurea |
| Molecular Formula | C15H23N7O4S |
| Purity | ≥95% |
| IUPAC Name | 1-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylurea |
| InChI | 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 |
| InChIKey | CACMCLIHCDTJHL-IDTAVKCVSA-N |
| SMILES | CCNC(=O)NCCSCC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)O |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
