Gambogic Acid

製品コードS2448 バッチS244804

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
* <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) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.
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. Gambogic Acid also blocks Kir2.1 channels with EC50 of ≤ 100 nM.[1] [2] [3] Gambogic Acid significantly inhibits human umbilical vein endothelial cell (HUVEC) proliferation, migration, invasion, tube formation, and micro-vessel growth at nM concentration. [4]
in vivo Gambogic Acid effectively inhibits tumor angiogenesis and suppressed tumor growth with low side effects using metronomic chemotherapy with Gambogic Acid. [4] Gambogic Acid has multiple functional effects including the induction of apoptosis, the inhibition of proliferation and the prevention of cancer metastasis and tumor angiogenesis. [5] In both animal tumor models and clinical trials, Gambogic Acid efficiently inhibits tumor growth with minimal side effects, with little toxicity on immune and hemopoietic systems. Gambogic Acid can produce tissue-specific proteasome inhibition and tumor-specific toxicity. [6] LD50: Mice 45mg/kg (i.p.). [7]

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.

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：

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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