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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-GSK3368715
GSK3368715

Chemical Structure : GSK3368715

CAS No.: 1629013-22-4

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GSK3368715 (EPZ019997,GSK-3368715)

货号: PC-72600Not For Human Use, Lab Use Only.

GSK3368715 (EPZ019997, GSK-3368715) is a potent, reversible and SAM uncompetitive type I PRMT inhibitor with Kiapp of 1.5 to 81 nM for PRMT1, 3, 4, 6, and 8.

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25 mg ￥3680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK3368715 (EPZ019997, GSK-3368715) is a potent, reversible and SAM uncompetitive type I PRMT inhibitor with Kiapp of 1.5 to 81 nM for PRMT1, 3, 4, 6, and 8.
GSK3368715 displays minimal inhibition against a panel of lysine methyltransferases, and no inhibition against type II and type III PRMTs.
GSK3368715 displays time-dependent inhibition of all the type I PRMTs except PRMT3, binds in the peptide site directly adjacent to the SAM pocket.
GSK3368715 demonstrated anti-proliferative activity against all cancer cell lines and primary patient samples; produces synergistic cancer cell growth inhibition when combined with PRMT5 inhibitor GSK3203591.
GSK3368715 induced an interferon gene signature, amplified responses to interferon and innate immune signaling pathways, and decreased expression of the immunosuppressive cytokine VEGF.

物理化学性质&存储条件

分子量 366.55
分子式 C20H38N4O2
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

N1-((3-(4,4-bis(ethoxymethyl)cyclohexyl)-1H-pyrazol-4-yl)methyl)-N1,N2-dimethylethane-1,2-diamine

参考文献

1. Fedoriw A, et al. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.

2. Noto PB, et al. Sci Rep. 2020 Dec 17;10(1):22155.

3. Fedoriw A, et al. Cancer Immunol Res. 2022 Feb 18:canimm.0614.2021.

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