research use only

Gambogic Acid Bcl-2 inhibitor

Name: Gambogic Acid
Brand: Selleck Chemicals
SKU: S2448
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S2448

Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, 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.

Chemical Structure

Molecular Weight: 628.75

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.42%

99.42

Related Targets	Apoptosis related Ras STAT TNF-alpha Caspase PD-1/PD-L1 Ferroptosis p53 RIP kinase c-RET MDM2/MDMX Myc Antifolate MRP IAP OXPHOS PERK FKBP Thymidylate Synthase ABC Transporter Heme Oxygenase PFKFB Pyroptosis Photosensitizer PKD Survivin Annexin A ASK Bcl-6 Nur77
Related Products	ABT-737 Navitoclax (ABT-263) Obatoclax Mesylate (GX15-070) S63845 A-1210477 TW-37 A-1331852 A-1155463 Dihydrochloride UMI-77 AZD5991 (R)-(-)-Gossypol (AT-101) acetic acid Sabutoclax WEHI-539 HA14-1 MIK665 (S64315) Obatoclax (GX15-070) Marinopyrrole A (Maritoclax) BAI1 A-1155463 BTSA1 S55746 Ruxotemitide (LTX 315) BAM7 BDA-366 Solanum lyratum Extract Bcl-2 Antibody [H20N17] Bcl-w Antibody [G2B1] BNIP3L/Nix Antibody [K19B13] APG-2575 (lisaftoclax) WH244

Chemical Information, Storage & Stability

Molecular Weight	628.75	Formula	C₃₈H₄₄O₈	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2752-65-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Guttatic Acid, Guttic Acid, Beta-Guttiferrin			Smiles	CC(=CCCC1(C=CC2=C(C3=C(C(=C2O1)CC=C(C)C)OC45C6CC(C=C4C3=O)C(=O)C5(OC6(C)C)CC=C(C)C(=O)O)O)C)C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (159.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
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.
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.
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.
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.
Clear solution	2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (6.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Bcl-w ^[1] 0.02 μM Bcl-B ^[1] 0.66 μM Mcl-1 ^[1] 0.79 μM Bfl-1 ^[1] 1.06 μM Bcl-2 ^[1] 1.21 μM Bcl-xL ^[1] 1.47 μM Caspase ^[1] <1.64 μM(EC50)
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.^[1] ^[2] ^[3] It 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 this compound. ^[4] It 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, 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. ^[6] LD50: Mice 45mg/kg (i.p.). ^[7]
References	[1] https://pubmed.ncbi.nlm.nih.gov/18566235/ [2] https://pubmed.ncbi.nlm.nih.gov/14723951/ [3] https://pubmed.ncbi.nlm.nih.gov/17673602/ [4] https://pubmed.ncbi.nlm.nih.gov/18339865/ [5] https://pubmed.ncbi.nlm.nih.gov/22339063/ [6] https://pubmed.ncbi.nlm.nih.gov/23260670/ [7] https://pubmed.ncbi.nlm.nih.gov/16918721/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):