Gambogic Acid

SKU: orb1301000

Description

Gambogic Acid is a natural small molecule that induces apoptosis by potently inhibiting anti-apoptotic Bcl-2 family proteins (Bcl-2, Bcl-XL, Mcl-1, etc.) and activating caspases (EC50 0.78-1.64 µM). It is widely used in cancer research, demonstrating antitumor activity in both cellular and animal models.

Research Area

Cell Biology

Key Properties

• CAS Number: 2752-65-0
• MW: 628.75
• Purity: 98.67%
• Formula: C₃₈H₄₄O₈
• SMILES: CC(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
• Target: Bcl-2 Family,Autophagy
• Solubility: H2O:Insoluble;DMSO:50 mg/mL (79.52 mM);Ethanol:62.9 mg/mL (100.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.18 mM)

Bioactivity

• Target IC50:
  BCL-W:2.02μM|BCL-B:0.66μM|BCL-XL:1.47μM|Bfl-1:1.06μM|Bcl-2:1.21μM|MCL1:0.79 μM
• In Vivo:
  Gambogic Acid effectively inhibits tumor angiogenesis and suppressed tumor growth with low side effects using metronomic chemotherapy with Gambogic Acid. Gambogic Acid 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 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. LD50: Mice 45 mg/kg (i.p.).
• 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. Gambogic Acid significantly inhibits human umbilical vein endothelial cell (HUVEC) proliferation, migration, invasion, tube formation, and micro-vessel growth at nM concentration.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

β-Guttiferrin, Beta-Guttiferrin, Autophagy, b-Guttiferrin, Bfl-1, Bcl-w, Bcl-B, Bcl-2, Bcl-2 Family, Inhibitor, Mcl-1, Guttatic Acid, Guttic Acid, Gambogic Acid, inhibit

Compound Identifiers

PubChem CID

5380091