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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
规格:98%
分子量:397.5
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)。
货号:ajcx20234
CAS:1674364-87-4
分子式:C15H23N7O4S
分子量:397.5
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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.

参考文献:
[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).