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1A-116

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].

Product Specifications

CAS Number

[1430208-73-3]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

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

99.72

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C16H16F3N3

Molecular Weight

307.31

Precautions

H315, H319, H335

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)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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