计算溶液所需的质量、体积或浓度。
概述
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 FOXP3
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 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 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-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.
IC50& Target:PRMT5 PRMT7
规格
规格或纯度
10mM in DMSO
英文名称
DS-437
生化机理
DS-437 是一种 PRMT5/7 双重抑制剂（PRMT5/7 的 IC 50 s=6 μM）。与其他 29 种人类蛋白质、DNA 和 RNA 甲基转移酶相比，DS-437 对 PRMT5 和 PRMT7 具有选择性。DS-437 是 PRMT5 的 S-腺苷蛋氨酸（SAM）竞争性抑制剂。DS-437 还能促进
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCNC(=O)NCCSC[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O
PubChem CID
分子量
397.45
高级数据
安全和危险性（GHS）
RIDADR
UN28116.1/PGIII
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）