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

Chemical Structure : Gambogenic acid

CAS No.: 173932-75-7

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Gambogenic acid (GNA)

货号: PC-35432Not For Human Use, Lab Use Only.

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells, specifically and covalently binds to Cys668 within the EZH2-SET domain.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells, specifically and covalently binds to Cys668 within the EZH2-SET domain.
Gambogenic acid specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=8.6 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
Gambogenic acid synergistically potentiates bortezomib-induced apoptosis in multiple myeloma.
Gambogenic acid also induces proteasomal degradation of CIP2A and sensitizes hepatocellular carcinoma to anticancer agents.

物理化学性质&存储条件

分子量 630.778
分子式 C38H46O8
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

(Z)-4-((1S,3aR,5S,12aS)-9-((E)-3,7-dimethylocta-2,6-dien-1-yl)-8,10-dihydroxy-2,2-dimethyl-11-(3-methylbut-2-en-1-yl)-4,7-dioxo-1,2,5,7-tetrahydro-1,5-methanofuro[2,3-d]xanthen-3a(4H)-yl)-2-methylbut-2-enoic acid

参考文献

1. Xu L, et al. Cell Death Dis. 2018 Feb 15;9(3):262.

2. Liu P, et al. J Cancer. 2017 Sep 16;8(16):3278-3286.

3. Wang X, et al. EMBO J. 2017 May 2;36(9):1243-1260.

4. Li F, et al. Exp Ther Med. 2017 May;13(5):2456-2462.

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