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ITX3

Cat. No. M7851
ITX3 Structure
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Biological Activity

ITX3 is a specific inhibitor of endogenous TrioN activity acting on the GEF domain and selective cell active inhibitor of the Trio/RhoG/Rac1 pathway. The compound is active in whole cell assay where it inhibits the formation of TrioN-dependent cell structures. ITX3 appears to be specific for TrioN inhibition rather than other RhoGEFs.

Chemical Information
Molecular Weight 371.45
Formula C22H17N3OS
CAS Number 347323-96-0
Solubility (25°C) DMSO: ≥4 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kiran A Vaidya, et al. Rac1 mediates Cadherin-11 induced cellular pathogenic processes in aortic valve calcification

[2] Shivangi, et al. A multifactorial assessment of the SRP pathway constituent FtsY as a vital mycobacterial constituent

[3] Kyonghee Son, et al. Supervillin binds the Rac/Rho-GEF Trio and increases Trio-mediated Rac1 activation

[4] Yan Yan, et al. Kalirin-9 and Kalirin-12 Play Essential Roles in Dendritic Outgrowth and Branching

[5] Nathalie Bouquier, et al. A cell active chemical GEF inhibitor selectively targets the Trio/RhoG/Rac1 signaling pathway

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