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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

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.

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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.
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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