Gambogic Acid

Catalog No.S2448 Synonyms: Guttatic Acid, Guttic Acid

Gambogic Acid Chemical Structure

Molecular Weight(MW): 628.75

Gambogic Acid 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.

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Biological Activity

Description Gambogic Acid 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.
Targets
Bcl-w [1] Bcl-B [1] Mcl-1 [1] Bfl-1 [1] Bcl-2 [1]
0.02 μM 0.66 μM 0.79 μM 1.06 μM 1.21 μM
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]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (159.04 mM)
Ethanol 100 mg/mL (159.04 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
4mg/mL

* 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.

Chemical Information

Molecular Weight 628.75
Formula

C38H44O8

CAS No. 2752-65-0
Storage powder
in solvent
Synonyms Guttatic Acid, Guttic Acid

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID