1A-116

• UNSPSC Description:

  1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo[1][2][3].

• Target Antigen:

  Apoptosis; Ras

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;GPCR/G Protein;MAPK/ERK Pathway

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/1A-116.html

• Purity:

  99.79

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  N=C(NC1=CC=CC=C1C(F)(F)F)NC2=CC(C)=CC(C)=C2

• Molecular Weight:

  307.31

• References & Citations:

  [1]Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840-51.|[2]Trebucq LL, et al. Timing of Novel Drug 1A-116 to Circadian Rhythms Improves Therapeutic Effects against Glioblastoma. Pharmaceutics. 2021 Jul 16;13(7):1091.|[3]González N, et al. Computational and in vitro Pharmacodynamics Characterization of 1A-116 Rac1 Inhibitor: Relevance of Trp56 in Its Biological Activity. Front Cell Dev Biol. 2020 Apr 15;8:240.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  1430208-73-3