.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsTW-37DMXAA (Vadimezan)Obatoclax mesylate (GX15-070)MethylprednisoloneTasisulamAdaroteneMolarity CalculatorDilution Calculator Gambogic AcidCaspase activator and apoptosis inducerCatalog No.A3424SizePriceStockQty10mM (in 1mL DMSO)$90.00In stock 5mg$65.00In stock 10mg$95.00In stock 25mg$145.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Publications citing ApexBio ProductsNature.2017 Jan 19;541(7637):417-420.Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Related Compound Libraries DiscoveryProbe™ Bioactive Compound LibraryDiscoveryProbe™ Ion Channel Compound LibraryDiscoveryProbe™ Apoptosis Compound LibraryQuality Control Quality Control & MSDS View current batch: 1 Purity = 98.54% COA (Certificate Of Analysis) HPLC (Retest) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Biological ActivityDescriptionGambogic Acid is an inducer of apoptosis with EC50 value of 0.78-1.64 μM for caspases and IC50 values of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1, respectively.TargetscaspasesBcl-XLBcl-2Bcl-WBcl-BBfl-1IC500.78-1.64 μM (EC50)1.47 μM1.21 μM2.02 μM0.66 μM1.06 μMProtocolCell experiment: [1]Cell linesMGC-803 cellsPreparation methodThe solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.Reaction Conditions1 μg/ml, 48 hApplicationsAfter exposure of MGC-803 cells to GA (1 μg/ml) for 24, 48, and 72 h, the apoptosis rate was 38.56, 73.70, and 71.77%, respectively. The proportion of G2/M phase cells increased after being treated with GA. Under an inverted-microscope, after cultured with GA 1 mg/ml for 48 h, many MGC-803 cells turned round in shape and necrosed; the untreated cells grew well and the skeleton was clear. Under electron microscope, “dotted” chromatins were found; in a large quantity of tumor cells these condensed chromatin divided into “Apoptosis bodies”.Animal experiment: [2]Animal modelsBALB/c nude mice bearing SMMC-7721 xenograftsDosage formIntravenous injection, 2, 4, and 8 mg/kg, 3 times per weekApplicationsThe results indicated that iv injection of GGA 2, 4, and 8 mg/kg inhibited dramatically the growth of human hepatocellular cell line SMMC-7721 in nude mice from the early administration.Other notesPlease test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.References: [1] Zhao L, Guo Q L, You Q D, et al. Gambogic acid induces apoptosis and regulates expressions of Bax and Bcl-2 protein in human gastric carcinoma MGC-803 cells. Biological and Pharmaceutical Bulletin, 2004, 27(7): 998-1003.[2] Guo Q L, You Q D, Wu Z Q, et al. General gambogic acids inhibited growth of human hepatoma SMMC-7721 cells in vitro and in nude mice. Acta Pharmacologica Sinica, 2004, 25: 769-774.Gambogic Acid Dilution CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateGambogic Acid Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate Chemical Properties Cas No. 2752-65-0SDF Download SDF Synonyms Beta-Guttiferrin,Gambogic Chemical Name (Z)-4-((1S,3aR,5S,11R,14aS)-8-hydroxy-2,2,11-trimethyl-13-(3-methylbut-2-en-1-yl)-11-(4-methylpent-3-en-1-yl)-4,7-dioxo-2,3a,4,5,7,11-hexahydro-1H-1,5-methanofuro[3,2-g]pyrano[3,2-b]xanthen-3a-yl)-2-methylbut-2-enoic acid Canonical SMILES C/C(C)=CCC[C@]1(C)C=CC(C(O)=C(C(C([C@]2([C@@H](C3)C(C)(C)O[C@]24C/C=C(C(O)=O)/C)O5)=C[C@H]3C4=O)=O)C5=C6C/C=C(C)C)=C6O1 Formula C38H44O8 M.Wt 628.75 Solubility ≥22.45 mg/mL in DMSO, ≥48.2 mg/mL in EtOH, Storage Store at -20°CPhysical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. BackgroundGambogic acid (GA) is an inducer of apoptosis with EC50 value of 0.78-1.64 μM for caspases and with IC50 values of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1, respectively [1].The cytotoxic natural product GA competes for BH3 peptide binding sites on several antiapoptotic members of the Bcl-2 family and neutralizes the ability of these proteins to suppress release of apoptogenic proteins from mitochondria.In vitro, it was demonstrated that GA inhibited the proliferation of human gastric carcinoma MGC-803 cells in a dose-dependent manner. When the cells were exposed to GA 5 mg/ml for 72 h, the rate of inhibition reached 89.45%. The IC50 value was 0.96 mg/ml at 48 h. In addition, GA can’t induce cell death in normal unimmortalized cells, but it can selectively kill the tumor cells. Treatment with GA at concentrations above 0.4 μM led to a significant dose-dependent inhibition of U266 cell growth under normoxia and hypoxia when U266 cells exposed to GA under normoxia and hypoxia for 8 h [2, 3].Using a prostate cancer xenograft model, s.c. injection daily for 15 days was reported that GA effectively inhibited tumor angiogenesis and suppressed tumor growth with few side effects. And using a mouse model of glioma, i.v. injection of GA daily for 14 days was reported to significantly reduce tumor volumes with little side effects. The effects of GA on expression of HIF-1a and its downstream target gene vascular endothelial growth factor was investigated in human MM U266 cells. Tumor xenografts transplanted by U266 cells were used to test the antitumor effect of GA in BALB ?c nude mice in vivo. After a treatment of 14-day, the tumors were moved and photographed. The results indicated that GA significantly inhibited tumor growth in a dosage-dependent manner. After exposure of MGC-803 cells to GA (1 μg/ml) for 24, 48, and 72 h, the apoptosis rate was 38.56, 73.70, and 71.77%, respectively. A number of MGC-803 cells turned round in shape and necrosed, while the untreated cells grew well and the skeleton was clear after cultured with GA 1mg/ml for 48 h [1, 3].References: [1].  Zhai DY, Jin CF, Shiau CW, et al. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Molecular Cancer Therapeutics, 2008, 7(6): 329-340.[2].  Zhao L, Guo QL, You QD, et al. Gambogic acid induces apoptosis and regulates expressions of Bax and Bcl-2 protein in human gastric carcinoma MGC-803 cells. Biological & Pharmaceutical Bulletin, 2004, 27(7): 998-1003.[3].  Wang F, Zhang W, Guo LT, et al. Gambogic acid suppresses hypoxia-induced hypoxia-inducible factor-1/vascular endothelial growth factor expression via inhibiting phosphatidylinositol 3-kinase/Akt/mammalian target protein of rapamycin pathway in multiple myeloma cells. Cancer Science, 2014, 105(8): 1063-1070.