1173671-63-0
Chemical Structure
Rhosin
- CAS No.: 1173671-63-0
- Formula:C20H18N6O
- Molecular Weight:358.40
IUPAC Name: (R,E)-2-amino-3-(1H-indol-3-yl)-N'-(quinoxalin-6-ylmethylene)propanehydrazide
InChIKey: FGYHLIHEFHCMPP-FVWOBLMASA-N
SMILES: O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4
Biological Activity: Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis[1][2]. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3].
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Rhosin | 98.74% | Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability. | ||||||||||||||||||||
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- [1]. Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710. [Content Brief]
- [2]. Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60. [Content Brief]
- [3]. Francis TC, et al. The Selective RhoA Inhibitor Rhosin Promotes Stress Resiliency Through Enhancing D1-Medium Spiny Neuron Plasticity and Reducing Hyperexcitability. Biol Psychiatry. 2019;85(12):1001-1010. [Content Brief]
Keywords
