DS-437
目录号: PL15081 纯度: ≥99%
CAS No. :1674364-87-4
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中文名称
DS-437
英文名称
DS-437
英文别名
BDBM50089221;1-(2-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)ethyl)-3-ethylurea;5 inverted exclamation marka-S-[2-[[(Ethylamino)carbonyl]amino]ethyl]-5 inverted exclamation marka-thioadenosine;1-[2-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylure;DS-437;5′-S-[2-[[(Ethylamino)carbonyl]amino]ethyl]-5′-thio-adenosine;5′-S-[2-[[(Ethylamino)carbonyl]amino]ethyl]-5′-thio-adenosine
Cas No.
1674364-87-4
分子式
C15H23N7O4S
分子量
397.45
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
DS-437 是双重蛋白精氨酸甲基转移酶 PRMT5/7 抑制剂,对两者的 IC50 均为 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 SAM 竞争性抑制剂。DS-437 还抑制 DNMT3A 和 DNMT3B,IC50 分别为 52 和 62 μM。DS-437 抑制 FOXP3 的甲基化。
生物活性
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.
性状
Solid
体外研究(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.
DS-437 increased total CD8 and CD8 PD-1 T cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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 antibody 4D5 had even more dramatic effects. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (314.50 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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