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Gambogic Acid

🥰Excellent
Catalog No. T6185Cas No. 2752-65-0
Alias Guttic Acid, Guttatic Acid, Beta-Guttiferrin

Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.

Gambogic Acid

Gambogic Acid

🥰Excellent
Purity: 98.67%
Catalog No. T6185Alias Guttic Acid, Guttatic Acid, Beta-GuttiferrinCas No. 2752-65-0
Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.
Pack SizePriceAvailabilityQuantity
2 mg$33 In Stock
5 mg$50 In Stock
10 mg$70 In Stock
25 mg$113 In Stock
50 mg$163 In Stock
100 mg$239 In Stock
500 mg$589 In Stock
1 mL x 10 mM (in DMSO)$80 In Stock
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Purity:98.67%
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Product Introduction

Bioactivity
Description
Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.
Targets&IC50
BCL-B:0.66μM, BCL-W:2.02μM, BCL-XL:1.47μM, BCL2:1.21μM, Bfl-1:1.06μM, MCL1:0.79 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 Clinicalal 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 45 mg/kg (i.p.). [7]
Kinase Assay
The fluorescence polarization reactions are performed. For Kidetermination, duplicate 200 μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R406 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R406, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally the apparent Km (or apparent Km/Vmax) is plotted against the inhibitor concentration to determine the Ki. All data analysis is performed using Prism and Prism enzyme kinetics programs[1]
AliasGuttic Acid, Guttatic Acid, Beta-Guttiferrin
Chemical Properties
Molecular Weight628.75
FormulaC38H44O8
Cas No.2752-65-0
SmilesCC(C)=CCCC1(C)OC2=C(CC=C(C)C)C3=C(C(O)=C2C=C1)C(=O)C1=CC2CC4C(C)(C)OC(C\C=C(/C)C(O)=O)(C2=O)C14O3
Relative Density.1.29 g/cm3
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: Insoluble
DMSO: 47.2 mg/mL (75.07 mM), Sonication is recommended.
Ethanol: 62.9 mg/mL (100.04 mM), Sonication is recommended.
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.5905 mL7.9523 mL15.9046 mL79.5229 mL
5 mM0.3181 mL1.5905 mL3.1809 mL15.9046 mL
10 mM0.1590 mL0.7952 mL1.5905 mL7.9523 mL
20 mM0.0795 mL0.3976 mL0.7952 mL3.9761 mL
50 mM0.0318 mL0.1590 mL0.3181 mL1.5905 mL
Ethanol
1mg5mg10mg50mg
100 mM0.0159 mL0.0795 mL0.1590 mL0.7952 mL

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