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DS-437
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DS-437图片
CAS NO:1674364-87-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
DS-437 是一种 PRMT5/7 双重抑制剂(PRMT5/7 的 IC50=6 μM)。
Cas No.1674364-87-4
化学名5'-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5'-thio-adenosine
Canonical SMILESO=C(NCC)NCCSC[C@@H]1[C@@H](O)[C@@H](O)[C@@](N2C3=NC=NC(N)=C3N=C2)([H])O1
分子式C15H23N7O4S
分子量397.5
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

DS-437 is a dual inhibitor of protein arginine methyltransferase 5 (PRMT5) and PRMT7 (IC50s = 5.9 and 6 μM, respectively).[1] It is selective for PRMT5 and PRMT7 over a panel of 29 additional protein, DNA, and RNA methyltransferases at 50 μM, but also inhibits DNMT3A and DNMT3B (IC50s = 52 and 62 μM, respectively). DS-437 (2.5 and 10 μM) inhibits symmetrical arginine dimethylation of FOXP3 in HEK293T cells, as well as symmetrical arginine dimethylation of p60 and the ribonucleoproteins SmD1/D3 and SmB/B’ in MDA-MB-231 cells in a concentration-dependent manner.[1],[2] It inhibits the ability of regulatory T cells (Tregs) to suppress effector T cell (Teff) proliferation in vitro in human and murine Treg suppression assays.[2] DS-437 (10 mg/kg five times per week) reduces tumor growth in a CT26Her2 murine colon cancer model when administered in combination with the anti-p185erbB2/neu antibody 4D5.

Reference:
[1]. Smil, D., Eram, M.S., Li, F., et al. Discovery of a dual PRMT5-PRMT7 inhibitor. ACS Med. Chem. Lett. 6(4), 408-412 (2015).
[2]. Nagai, Y., Ji, M.Q., Zhu, F., et al. PRMT5 associates with the FOXP3 homomer and when disabled enhances targeted p185erbB2/neu tumor immunotherapy. Front. Immunol. 10:174, (2019).