Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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Purity: ≥98%
Gambogenic Acid, a naturally occuring ingredient dound in gamboge, is a potent inhibitor of the fibroblast growth factor receptor (FGFR) signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC). It can inhibit the growth of xenografts derived from patients and exhibit anticancer properties. Gambogenic acid specifically and covalently binds to Cys668 within the EZH2-SET domain, causing EZH2 ubiquitination, thereby acting as an effective inhibitor of EZH2.
Targets |
FGFR; EZH2
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ln Vitro |
Gambogenic acid is a novel agent that specifically and covalently binds to Cys668 within the EZH2‐SET domain, causing EZH2 degradation through ubiquitination at the COOH terminus of the Hsp70-interacting protein (CHIP). Gambogenic acid effectively reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes and significantly suppresses H3K27Me3. In an EZH2-dependent manner, gambogenic acid significantly suppresses the growth of tumors.[1]
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ln Vivo |
Gambogenic acid derivative GNA002 dramatically lowers H3K27Me3 levels in tumor tissues and the volumes of tumors derived from Cal-27 in xenograft mice.
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Cell Assay |
GNA002 or 2 μM GNA is applied to cancer cells for a full day. Subsequently, the cells are collected and mixed again with 500 μl of binding buffer. Different cell dyes are added to the 100 μl of cell suspension and incubated. Fluorescence-activated cell sorting is used to analyze the stained cells using a flow cytometry apparatus.
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References |
Molecular Formula |
C38H46O8
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Molecular Weight |
630.7671
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Exact Mass |
630.32
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Elemental Analysis |
C, 72.36; H, 7.35; O, 20.29
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CAS # |
173932-75-7
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Related CAS # |
173932-75-7
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Appearance |
Solid powder
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SMILES |
CC(=CCC/C(=C/CC1=C(C(=C2C(=C1O)C(=O)C3=C[C@@H]4C[C@@H]5[C@@]3(O2)[C@](C4=O)(OC5(C)C)C/C=C(/C)\C(=O)O)CC=C(C)C)O)/C)C
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InChi Key |
RCWNBHCZYXWDOV-VSFMGBBVSA-N
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InChi Code |
InChI=1S/C38H46O8/c1-20(2)10-9-11-22(5)13-15-25-30(39)26(14-12-21(3)4)33-29(31(25)40)32(41)27-18-24-19-28-36(7,8)46-37(34(24)42,38(27,28)45-33)17-16-23(6)35(43)44/h10,12-13,16,18,24,28,39-40H,9,11,14-15,17,19H2,1-8H3,(H,43,44)/b22-13+,23-16-/t24-,28+,37+,38-/m1/s1
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Chemical Name |
(Z)-4-[(1S,2S,13S,15R)-7-[(2E)-3,7-dimethylocta-2,6-dienyl]-6,8-dihydroxy-17,17-dimethyl-5-(3-methylbut-2-enyl)-10,14-dioxo-3,16-dioxapentacyclo[11.4.1.02,11.02,15.04,9]octadeca-4,6,8,11-tetraen-15-yl]-2-methylbut-2-enoic acid
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Synonyms |
GNA; Gambogenic Acid
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~158.5 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5854 mL | 7.9268 mL | 15.8536 mL | |
5 mM | 0.3171 mL | 1.5854 mL | 3.1707 mL | |
10 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Screening and identification of gambogenic acid (GNA) to directly interact with EZH2. EMBO J . 2017 May 2;36(9):1243-1260. td> |