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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-C220
C220

Chemical Structure : C220

CAS No.: 1989620-03-2

C220 (PRMT5 inhibitor C220)

货号: PC-21273Not For Human Use, Lab Use Only.

C220 (PRMT5 inhibitor C220) is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 2.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

C220 (PRMT5 inhibitor C220) is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 2.4 nM.
C220 reduces mouse and human allogeneic T cell proliferation and inflammatory IFN-γ and IL-17 cytokine production.
C220 improves survival, reducing disease incidence and clinical severity in mouse models of aGVHD without adversely affecting engraftment in vivo.
C220 deregulates the cell cycle in activated T cells and disrupts signaling by affecting ERK1/2 phosphorylation.
C220 broadly suppresses DDR Gene expression in ovarian and breast cancer cells, C220 dysregulates chromatin- and splicing-mediated regulation of DDR pathways.
C220 induces DNA repair deficiency, and synergizes with PARP inhibition and chemotherapy in vitro and in vivo.

物理化学性质&存储条件

分子量 376.80
分子式 C17H17ClN4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R,3R,4S,5R)-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-((R)-(4-chlorophenyl)(hydroxy)methyl)tetrahydrofuran-3,4-diol

参考文献

1. Katiri J Snyder, et al. JCI Insight. 2020 Apr 23;5(8):e131099.

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