645890

Trio N-Terminal RhoGEF Domain Inhibitor, ITX3

The Trio N-Terminal RhoGEF Domain Inhibitor, ITX3, also referenced under CAS 347323-96-0, controls the biological activity of Trio N-Terminal RhoGEF Domain. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): Trio N-Terminal RhoGEF Domain Inhibitor, ITX3, (2E)-(-2-((2,5-Dimethyl-1-phenyl-pyrrol-3-yl)methylene)thiazolo[3,2-a]benzimidazol-1-one, Inhibitor of Ttrio e Xchange 3
• Empirical Formula (Hill Notation): C₂₂H₁₇N₃OS
• CAS Number: 347323-96-0
• Molecular Weight: 371.45
• MDL number: MFCD02629172
• UNSPSC Code: 12352200
• NACRES: NA.32

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 2 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C22H17N3OS/c1-14-12-16(15(2)24(14)17-8-4-3-5-9-17)13-20-21(26)25-19-11-7-6-10-18(19)23-22(25)27-20/h3-13H,1-2H3/b20-13+
• InChI key: SJMYMKPBODEZSH-DEDYPNTBSA-N

Description

General description

A cell-permeable thiazolo-benzimidazolone compound that inhibits Trio N-terminal RhoGEF domain- (TrioN) mediated RhoG activation (IC₅₀ = 76 µM) and effectively reduces cellular Rac activation (by 80% with 50 µM ITX3) caused by TrioN, but not GEF337 (RhoA GEF), Tiam1 (Rac GEF), or Vav2 (Rac1/RhoA/Cdc42 GEF), overexpression in HEK293T cells. Culture treatment of ITX at 100 µM is shown to reduce NGF-induced neurite outgrowth of rat PC12 pheochromocytoma cells by 50% and block the formation of multinucleated myotubes by 78% in C2C12 mouse myoblasts cultures induced for differentiation, while the differentiation-associated Myogenin and Troponin T expressions in Trio knock-down C2C12 cells are not affected by ITX at the same concentration.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Bouquier, N., et al. 2009. Chem. Biol.16, 657.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable