For research use only. Not for therapeutic Use.
Gambogic acid (CAT: I002945) has been found to exert its anticancer effects through the modulation of B-cell lymphoma 2 (BCL-2) family proteins. BCL-2 family proteins play a critical role in regulating apoptosis (programmed cell death). Gambogic acid has been shown to induce apoptosis in cancer cells by inhibiting anti-apoptotic proteins such as BCL-2 and BCL-XL while promoting the expression of pro-apoptotic proteins like BAX and BAK. This imbalance in the expression of BCL-2 family proteins leads to mitochondrial dysfunction and activation of caspases, ultimately triggering apoptosis in cancer cells. The ability of gambogic acid to target BCL-2 family proteins makes it a promising candidate for the development of novel anticancer therapies.
| Catalog Number | I002945 |
| CAS Number | 2752-65-0 |
| Synonyms | (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 |
| Molecular Formula | C38H44O8 |
| Purity | ≥95% |
| Target | Caspase |
| Solubility | DMSO 25 mg/ml; water <1 mg/ml |
| Storage | 3 years -20C powder |
| IC50 | 1.21 uM (Bcl-2); 1.47 uM (Bcl-xl) |
| InChI | InChI=1S/C38H44O8/c1-20(2)10-9-15-36(8)16-14-24-29(39)28-30(40)26-18-23-19-27-35(6,7)46-37(33(23)41,17-13-22(5)34(42)43)38(26,27)45-32(28)25(31(24)44-36)12-11-21(3)4/h10-11,13-14,16,18,23,27,39H,9,12,15,17,19H2,1-8H3,(H,42,43)/b22-13-/t23-,27+,36-,37+,38- |
| InChIKey | GEZHEQNLKAOMCA-RRZNCOCZSA-N |
| SMILES | C/C(C(O)=O)=C/C[C@@]1(OC(C)(C)[C@]2([H])C3)[C@@]2(OC4=C(C5=C6C=C[C@](CC/C=C(C)/C)(C)O5)C/C=C(C)/C)C(C(C4=C6O)=O)=C[C@@]3([H])C1=O |
| Reference | </br>1:Gambogic acid suppresses cancer invasion and migration by inhibiting TGFβ1-induced epithelial-to-mesenchymal transition. Zhao K, Zhang S, Song X, Yao Y, Zhou Y, You Q, Guo Q, Lu N.Oncotarget. 2017 Apr 18;8(16):27120-27136. doi: 10.18632/oncotarget.15449. PMID: 28404892 Free PMC Article</br>2:Inhibition of inwardly rectifying Kir2.x channels by the novel anti-cancer agent gambogic acid depends on both pore block and PIP<sub>2</sub> interference. Scherer D, Schworm B, Seyler C, Xynogalos P, Scholz EP, Thomas D, Katus HA, Zitron E.Naunyn Schmiedebergs Arch Pharmacol. 2017 Apr 2. doi: 10.1007/s00210-017-1372-5. [Epub ahead of print] PMID: 28365825 </br>3:Gambogic acid potentiates the chemosensitivity of colorectal cancer cells to 5-fluorouracil by inhibiting proliferation and inducing apoptosis. Wei J, Yang P, Li W, He F, Zeng S, Zhang T, Zhong J, Huang D, Chen Z, Wang C, Chen H, Hu H, Cao J.Exp Ther Med. 2017 Feb;13(2):662-668. doi: 10.3892/etm.2017.4021. Epub 2017 Jan 2. PMID: 28352348 Free PMC Article</br>4:Gambogic acid-loaded biomimetic nanoparticles in colorectal cancer treatment. Zhang Z, Qian H, Yang M, Li R, Hu J, Li L, Yu L, Liu B, Qian X.Int J Nanomedicine. 2017 Feb 28;12:1593-1605. doi: 10.2147/IJN.S127256. eCollection 2017. PMID: 28280328 Free PMC Article</br>5:Gambogic acid grafted low molecular weight heparin micelles for targeted treatment in a hepatocellular carcinoma model with an enhanced anti-angiogenesis effect. Yan X, Yang Y, He L, Peng D, Yin D.Int J Pharm. 2017 Apr 30;522(1-2):110-118. doi: 10.1016/j.ijpharm.2017.02.051. Epub 2017 Feb 24. PMID: 28242375 </br>6:Triphenylphosphonium-modified poly(ethylene glycol)-poly(ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery. Xu Y, Wang S, Chan HF, Liu Y, Li H, He C, Li Z, Chen M.Int J Pharm. 2017 Apr 30;522(1-2):21-33. doi: 10.1016/j.ijpharm.2017.01.064. Epub 2017 Feb 12. PMID: 28215509 </br>7:Gambogic acid inhibits the growth of ovarian cancer tumors by regulating p65 activity. Tang Q, Lu M, Zhou H, Chen D, Liu L.Oncol Lett. 2017 Jan;13(1):384-388. doi: 10.3892/ol.2016.5433. Epub 2016 Nov 24. PMID: 28123571 Free PMC Article</br>8:Role of gambogic acid and NaI<sup>131</sup> in A549/DDP cells. Huang J, Zhu X, Wang H, Han S, Liu L, Xie Y, Chen D, Zhang Q, Zhang L, Hu Y.Oncol Lett. 2017 Jan;13(1):37-44. doi: 10.3892/ol.2016.5435. Epub 2016 Nov 25. PMID: 28123519 Free PMC Article</br>9:Development of a More Efficient Albumin-Based Delivery System for Gambogic Acid with Low Toxicity for Lung Cancer Therapy. Zhang Y, Yang Z, Tan X, Tang X, Yang Z.AAPS PharmSciTech. 2016 Dec 8. [Epub ahead of print] PMID: 27933587 </br>10:Gambogic acid counteracts mutant p53 stability by inducing autophagy. Foggetti G, Ottaggio L, Russo D, Monti P, Degan P, Fronza G, Menichini P.Biochim Biophys Acta. 2017 Feb;1864(2):382-392. doi: 10.1016/j.bbamcr.2016.11.023. Epub 2016 Nov 27. PMID: 27899303 |
