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Bragsin1

Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity[1].

Product Specifications

CAS Number

[369631-68-5]

UNSPSC

12352005

Target

Arf Family GTPase

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Bragsin1.html

Concentration

10mM

Purity

99.91

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

Smiles

O=C1C=C(C(F)(F)F)OC2=CC=C(C)C([N+]([O-])=O)=C21

Molecular Formula

C11H6F3NO4

Molecular Weight

273.16

References & Citations

[1]Nawrotek A, et al. PH-domain-binding inhibitors of nucleotide exchange factor BRAG2 disrupt Arf GTPase signaling. Nat Chem Biol. 2019 Feb 11. doi: 10.1038/s41589-019-0228-3.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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