| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
ArfGEF BRAG2 (Brefeldin A-resistant Arf guanine nucleotide exchange factor 2). Bragsin2 is a selective, non-competitive inhibitor of BRAG2. It binds at the interface between the PH domain of BRAG2 and the lipid bilayer. It inhibits Arf GTPase activation with an IC50 of 3 microM.
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| ln Vitro |
HeLa cells' Arf GTPase activation is inhibited by bragsin2 (50 μM) [1]. SUM149 and S68 cannot grow when bragsin2 (50 μM) is present; however, SUM159, which lacks adhesion molecules like integrins and cadherins, is unaffected [1].
Bragsin2 inhibits Arf GTPase activation with an IC50 of 3 microM. It is a potent, selective, and noncompetitive inhibitor of the nucleotide exchange factor BRAG2. The compound binds at the interface between the PH domain of BRAG2 and the lipid bilayer, preventing BRAG2 from activating lipidated Arf GTPase. It affects the trans-Golgi network in a BRAG2- and Arf-dependent manner in cells. |
| ln Vivo |
No specific in vivo activity data is available for Bragsin2. Based on its inhibition of BRAG2, it has potential for in vivo studies in cancer models. Bragsin2 is a precise small-molecule probe for dissecting BRAG2-membrane coupling, Arf regulation, and adhesion-dependent cancer signaling.
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| Enzyme Assay |
In vitro enzyme assays for Bragsin2 involve measuring its inhibition of BRAG2-mediated Arf GTPase activation. The assay typically uses purified BRAG2 protein and Arf GTPase in the presence of membranes or lipid vesicles, as Bragsin2 requires the lipid bilayer for its inhibitory activity. GTP loading on Arf is measured, and the IC50 is determined from dose-response curves.
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| Cell Assay |
The in vitro cellular activity of Bragsin2 is evaluated in cells expressing BRAG2. Cells are treated with the compound, and Arf GTPase activation is measured using pull-down assays. The compound's effects on the trans-Golgi network and other BRAG2-dependent cellular processes are assessed. Bragsin2 is used to study BRAG2 function in cancer biology and membrane trafficking pathways.
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| Animal Protocol |
No specific in vivo animal experimental protocols are available for Bragsin2. Based on its role in cancer signaling, potential in vivo studies would involve xenograft mouse models where tumor-bearing mice are administered Bragsin2 via intraperitoneal injection or oral gavage. Dosing regimens and endpoints would be determined based on the specific study objectives.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data is available for Bragsin2. As a small molecule (molecular weight 273.16, formula C11H6F3NO4), it is expected to have moderate lipophilicity and cell permeability. The compound is hydration-resistant, suggesting stability in aqueous environments. Solubility: DMSO. Storage: powder at -20degC for 3 years.
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| Toxicity/Toxicokinetics |
No specific toxicological data is available for Bragsin2. As a research compound intended for laboratory use, standard safety precautions should be observed. No clinical toxicity studies have been reported. The compound has not been evaluated for genotoxicity, carcinogenicity, or reproductive toxicity.
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| References | |
| Additional Infomation |
Bragsin2 is a hydration-resistant, cell-permeant, selective, non-competitive inhibitor of BRAG2 with an IC50 of 3 microM. It binds at the BRAG2 PH domain-lipid bilayer interface and is a probe for studying BRAG2-membrane coupling, Arf regulation, and cancer signaling. It is not approved for clinical use.
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| Molecular Formula |
C11H6F3NO5
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| Molecular Weight |
289.1643
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| Exact Mass |
289.02
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| Elemental Analysis |
C, 45.69; H, 2.09; F, 19.71; N, 4.84; O, 27.66
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| CAS # |
342795-08-8
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| PubChem CID |
799794
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C2=C(C=C1)OC(=CC2=O)C(F)(F)F)[N+](=O)[O-]
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| InChi Key |
WJUILHMXVGFAIS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H6F3NO5/c1-19-7-3-2-6-9(10(7)15(17)18)5(16)4-8(20-6)11(12,13)14/h2-4H,1H3
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| Chemical Name |
6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one
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| Synonyms |
Bragsin2; Bragsin-2; Bragsin 2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~345.83 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4583 mL | 17.2915 mL | 34.5829 mL | |
| 5 mM | 0.6917 mL | 3.4583 mL | 6.9166 mL | |
| 10 mM | 0.3458 mL | 1.7291 mL | 3.4583 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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