Gambogic Acid

製品コードS2448 バッチS244802

印刷

化学情報

Chemical Structure Synonyms Guttatic Acid, Guttic Acid, Beta-Guttiferrin Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C38H44O8
分子量 628.75 CAS No. 2752-65-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (159.04 mM)
Ethanol 100 mg/mL (159.04 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Gambogic Acid (Guttatic Acid、Guttic Acid、Beta-Guttiferrin) は、0.78-1.64 µM の EC50 でカスパーゼを活性化し、Bcl-XL、Bcl-2、Bcl-W、Bcl-B、Bfl-1、Mcl-1 をそれぞれ 1.47、1.21、2.02、0.66、1.06、0.79 µM の IC50 で競合的に阻害します。
in vitro Gambogic Acid is a caged xanthone that is derived from Garcinia hanburyi and functions as a strong apoptotic inducer in many types of cancer cells by inhibiting human Bcl-2 family proteins and activating caspases. This compound also blocks Kir2.1 channels with EC50 of ≤ 100 nM. It significantly inhibits human umbilical vein endothelial cell (HUVEC) proliferation, migration, invasion, tube formation, and micro-vessel growth at nM concentration.
in vivo Gambogic Acid effectively inhibits tumor angiogenesis and suppressed tumor growth with low side effects using metronomic chemotherapy with this compound. It has multiple functional effects including the induction of apoptosis, the inhibition of proliferation and the prevention of cancer metastasis and tumor angiogenesis. In both animal tumor models and clinical trials, this agent efficiently inhibits tumor growth with minimal side effects, with little toxicity on immune and hemopoietic systems. This chemical can produce tissue-specific proteasome inhibition and tumor-specific toxicity. LD50: Mice 45mg/kg (i.p.).

プロトコル(参考用のみ)

キナーゼアッセイ Competitive peptide displacement assay
GST-Bcl-2 or other GST tagged human Bcl-2 family proteins (100 nmol/L) are incubated with Gambogic Acid at various concentrations for 5 min at room temperature in PBS. Then, 5 nmol FITC-Bid BH3 peptide is added and fluorescence polarization is measured after 10min. IC50 determinations are generated by fitting the experimental data using a sigmoidal dose-response nonlinear regression model.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18566235/
  • https://pubmed.ncbi.nlm.nih.gov/14723951/
  • https://pubmed.ncbi.nlm.nih.gov/17673602/
  • https://pubmed.ncbi.nlm.nih.gov/18339865/
  • https://pubmed.ncbi.nlm.nih.gov/22339063/
  • https://pubmed.ncbi.nlm.nih.gov/23260670/
  • https://pubmed.ncbi.nlm.nih.gov/16918721/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

TMTP1-modified nanocarrier boosts cervical cancer immunotherapy by eliciting pyroptosis [ Theranostics, 2025, 15(11):5420-5439] PubMed: 40303327
Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy [ Cells, 2023, 12(18)2247] PubMed: 37759469
Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy [ Cells, 2023, 10.3390/cells12182247] PubMed: 37759469
Gambogic Acid Induces Pyroptosis of Colorectal Cancer Cells through the GSDME-Dependent Pathway and Elicits an Antitumor Immune Response [ Cancers (Basel), 2022, 14(22)5505] PubMed: 36428598
Identification of Therapeutic Vulnerabilities in Small Cell Neuroendocrine Prostate Cancer. [ Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775] PubMed: 31806643

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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