| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ArfGEF BRAG2 (Brefeldin A-resistant Arf guanine nucleotide exchange factor 2, also known as IQSEC2). Bragsin1 inhibits BRAG2-mediated Arf GTPase activation by targeting the PH domain of BRAG2. It is a noncompetitive inhibitor with an IC50 of 3 microM.
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| ln Vitro |
Bragsin1 inhibits Arf GTPase activation with an IC50 of 3 microM. It is a potent and selective inhibitor of BRAG2, targeting the PH domain of BRAG2 in vitro and in cells. It inhibits BRAG2-mediated Arf GTPase activation in a manner that requires a membrane. Bragsin1 has anti-cancer activity.
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| ln Vivo |
No specific in vivo activity data is available for Bragsin1. Its anti-cancer activity suggests potential for in vivo efficacy studies in cancer models. As a research tool for studying BRAG2 function, it is primarily used in cell-based assays to investigate Arf signaling and membrane trafficking.
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| Enzyme Assay |
In vitro enzyme assays for Bragsin1 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, as Bragsin1 requires a membrane for its inhibitory activity. GTP loading on Arf is measured using radioactive or fluorescent GTP analogs, and the IC50 is determined from dose-response curves.
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| Cell Assay |
The in vitro cellular activity of Bragsin1 is evaluated in cells expressing BRAG2. Cells are treated with varying concentrations of Bragsin1, and Arf GTPase activation is measured using pull-down assays with GST-fused effector domains that specifically bind active Arf-GTP. The compound's ability to inhibit BRAG2-mediated Arf activation in cells is assessed, with effects on downstream signaling and cellular phenotypes also examined.
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| Animal Protocol |
No specific in vivo animal experimental protocols are available for Bragsin1. Based on its anti-cancer activity, potential in vivo studies would involve xenograft mouse models where tumor-bearing mice are administered Bragsin1 via intraperitoneal injection or oral gavage. Dosing regimens and endpoints (tumor volume, body weight, survival) would be determined based on the specific study objectives.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data is available for Bragsin1. As a small molecule (molecular weight 273.16, formula C11H6F3NO4), it is expected to have moderate lipophilicity and potential for cell penetration. Solubility: DMSO 62.5 mg/mL (228.80 mM). Storage: powder at -20degC.
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| Toxicity/Toxicokinetics |
No specific toxicological data is available for Bragsin1. 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 |
Bragsin1 is a potent, selective, noncompetitive inhibitor of the ArfGEF BRAG2, inhibiting Arf GTPase activation with an IC50 of 3 microM. It has anti-cancer activity. The compound is a research tool for dissecting BRAG2-membrane coupling, Arf regulation, and adhesion-dependent cancer signaling. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C11H6F3NO4
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|---|---|
| Molecular Weight |
273.164853572845
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| Exact Mass |
273.024
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| CAS # |
369631-68-5
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| PubChem CID |
740511
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| Appearance |
White to off-white solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C2=C(C=C1)OC(=CC2=O)C(F)(F)F)[N+](=O)[O-]
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| InChi Key |
WEUSXIBCGCFOQR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H6F3NO4/c1-5-2-3-7-9(10(5)15(17)18)6(16)4-8(19-7)11(12,13)14/h2-4H,1H3
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| Chemical Name |
6-methyl-5-nitro-2-(trifluoromethyl)chromen-4-one
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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 : ~62.5 mg/mL (~228.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6609 mL | 18.3043 mL | 36.6086 mL | |
| 5 mM | 0.7322 mL | 3.6609 mL | 7.3217 mL | |
| 10 mM | 0.3661 mL | 1.8304 mL | 3.6609 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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