Gambogenic acid
Gambogenic acid Basic information
- Product Name:
- Gambogenic acid
- Synonyms:
-
- Gambogenic acid
- (2Z)-4-[(1R,3aS,5S,12aS)-9-[(2E)-3,7-Dimethyl-2,6-octadien-1-yl]-3a,4,5,7-tetrahydro-8,10-dihydroxy-3,3-dimethyl-11-(3-methyl-2-buten-1-yl)-7,13-dioxo-1,5-methano-1H,3H-furo[3,4-d]xanthen-1-yl]-2-methyl-2-butenoic acid
- 2-Butenoic acid, 4-[(1R,3aS,5S,12aS)-9-[(2E)-3,7-dimethyl-2,6-octadien-1-yl]-3a,4,5,7-tetrahydro-8,10-dihydroxy-3,3-dimethyl-11-(3-methyl-2-buten-1-yl)-7,13-dioxo-1,5-methano-1H,3H-furo[3,4-d]xanthen-1-yl]-2-methyl-, (2Z)-
- Gambogenic acid,Histone Methyltransferase,inhibit,Inhibitor
- (Z)-4-((1R,3aS,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
- Gambogenic acid, 10 mM in DMSO
- CAS:
- 173932-75-7
- MF:
- C38H46O8
- MW:
- 630.78
- Mol File:
- 173932-75-7.mol
Gambogenic acid Chemical Properties
- Boiling point:
- 818.6±65.0 °C(Predicted)
- Density
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO : 250 mg/mL (396.34 mM; Need ultrasonic)
- form
- Powder
- pka
- 4.58±0.36(Predicted)
- color
- Light yellow to yellow
Gambogenic acid Usage And Synthesis
Chemical Properties
Brown-red crystalline powder, soluble in organic solvents such as methanol, ethanol, and DMSO, derived from Garcinia.
Uses
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer[1][2].
in vivo
Gambogenic acid (4-12 mg/kg, i.v., every 2 days, 14 days) inhibits tumor growth in SCLC mouse xenograft model[2].
| Animal Model: | SCLC mouse xenograft model[1] |
| Dosage: | 4-12 mg/kg |
| Administration: | i.v., every 2 days, 14 days |
| Result: | Increased the expression of pro-apoptotic proteins (cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins). Decreased the anti-apoptotic proteins (Bcl-2). |
IC 50
EZH2
References
[1] Wang X, et al. A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination. EMBO J. 2017 May 2;36(9):1243-1260. DOI:10.15252/embj.201694058
[2] Huang T, et al. Gambogenic acid inhibits the proliferation of small?cell lung cancer cells by arresting the cell cycle and inducing apoptosis. Oncol Rep. 2019 Mar;41(3):1700-1706. DOI:10.3892/or.2018.6950
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