DS-437 (C09-1125-592)

DS-437 is a dual PRMT5/7 inhibitor ( IC 50 s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5 . DS-437 also inhibits DNMT3A and DNMT3B, with IC 50 s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3In VitroDS-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 IC 50 ?of 5.9 ± 1.4 μM. ?/nDS-437 increased total CD8 + ?and CD8 + PD-1 + T cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoDS-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-p185 erbB2/neu ?antibody 4D5 had even more dramatic effects . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six to Ten weeks old female Balb/c mice (bearing  CT26Her2 tumor cells) Dosage: 10 mg/kg Administration: i.p.; 5 times a week Result: Had some beneficial effects on inhibiting tumor growth.Form:SolidIC50& Target:PRMT5 PRMT7. Specifications and Purity: 98%. Molecular Formula: C15H23N7O4S. Molecular Weight: 397.45. PubChem CID: 122178085. Isomeric SMILES: CCNC(=O)NCCSC[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O.