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ITX 3

Names

[ CAS No. ]:
347323-96-0

[ Name ]:
ITX 3

Biological Activity

[Description]:

ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.IC50 value: 76 uM [1]Target: TrioN inhibitorIn transfected mammalian cells, ITX3 blocked TrioN-mediated dorsal membrane ruffling and Rac1 activation while having no effect on GEF337-, Tiam1-, or Vav2-mediated RhoA or Rac1 activation. ITX3 specifically inhibited endogenous TrioN activity, as evidenced by its ability to inhibit neurite outgrowth in nerve growth factor (NGF)–stimulated PC12 cells or C2C12 differentiation into myotubes [1]. ITX3 repressed the Rac1 activity and dose dependently up-regulated the E-cadherin protein level in the Tara-KD cells [2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Others

[References]

[1]. Bouquier N, et al. A cell active chemical GEF inhibitor selectively targets the Trio/RhoG/Rac1 signaling pathway. Chem Biol. 2009 Jun 26;16(6):657-66.

[2]. Yano T, et al. Tara up-regulates E-cadherin transcription by binding to the Trio RhoGEF and inhibiting Rac signaling. J Cell Biol. 2011 Apr 18;193(2):319-32.


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Molecular Formula ]:
C22H17N3OS

[ Molecular Weight ]:
371.45500

[ Exact Mass ]:
371.10900

[ PSA ]:
67.54000

[ LogP ]:
3.86440

[ Storage condition ]:
2-8℃

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

A local VE-cadherin and Trio-based signaling complex stabilizes endothelial junctions through Rac1.

J. Cell Sci. 128 , 3041-54, (2015)

Endothelial cell-cell junctions maintain a restrictive barrier that is tightly regulated to allow dynamic responses to permeability-inducing angiogenic factors, as well as to inflammatory agents and a...

The Rho-GEF Trio regulates a novel pro-inflammatory pathway through the transcription factor Ets2.

Biol. Open 2 , 569-79, (2013)

Inflammation is characterized by endothelium that highly expresses numerous adhesion molecules to trigger leukocyte extravasation. Central to this event is increased gene transcription. Small Rho-GTPa...


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Related Compounds