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Chemical Structure| 1281870-42-5 Chemical Structure| 1281870-42-5

Structure of Rhosin HCl
CAS No.: 1281870-42-5

Chemical Structure| 1281870-42-5

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Rhosin HCl is a specific Rho inhibitor which binds to WT RhoA with an affinity ~0.4 μM Kd while does not interfere with the binding of Cdc42 or Rac1.

Synonyms: Rhosin (hydrochloride); Rhosin hydrochloride; G04

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Product Details of Rhosin HCl

CAS No. :1281870-42-5
Formula : C20H19ClN6O
M.W : 394.86
SMILES Code : O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4.[H]Cl
Synonyms :
Rhosin (hydrochloride); Rhosin hydrochloride; G04
MDL No. :MFCD18794648
InChI Key :SFRGBDFQSLZYLF-GRYLRVQNSA-N
Pubchem ID :52998412

Safety of Rhosin HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human platelets 20 µM 2 min Blocked the phosphorylation of the myosin light chain (p-MLC) PMC9961652
PC-3 cells 30 μM RhoA inhibitor Rhosin diminished CRMP4a shRNA-induced increase of cancer cell migration PMC6301799
Rat bone marrow mesenchymal stem cells 20 μM 14 days To investigate the effect of Rhosin on the proliferation and osteogenic differentiation of BMSC under dynamic culture conditions. Results showed that Rhosin inhibited the proliferation and osteogenic differentiation of BMSC. PMC10189446
Human lung microvascular endothelial cells (HLMVEC) 30 μM 2 hours To investigate the inhibitory effect of Rhosin on 2-ClHA-induced endothelial barrier dysfunction. Results showed that Rhosin pretreatment significantly inhibited the barrier dysfunction caused by 2-ClHA. PMC11979405
HEK293 cells 5µM, 10µM, 15µM, 30µM 2 hours To investigate the effect of Rhosin on F/G-actin ratio in GNE mutant cells. Results showed that treatment with 10µM Rhosin restored the F/G-actin ratio in GNE mutant cells. PMC8012676
4T1 cells 1-50 μM 3 days Rhosin inhibited RhoA and RhoC activation, and suppressed YAP nuclear localization, but did not affect ERK1/2, Akt, or NF-κB activation. PMC7824767
B16BL6 cells 1-50 μM 3 days Rhosin inhibited RhoA and RhoC activation, and suppressed YAP nuclear localization, but did not affect ERK1/2, Akt, or NF-κB activation. PMC7824767

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Chronic social defeat stress model Intraperitoneal injection 40 mg/kg Once daily for 7 days To evaluate the effects of Rhosin on behavioral and physiological changes induced by chronic social defeat stress, it was found that Rhosin prevented social avoidance and reduced sucrose preference caused by CSDS, and enhanced spine density in D1-MSNs. PMC7368664
C57BL/6J mice and Balb/c mice B16BL6 and 4T1 lung metastasis model Intraperitoneal injection 10 mg/kg or 30 mg/kg Daily for 14 days Rhosin reduced the number of lung metastatic nodules in B16BL6 and 4T1 cells in a dose-dependent manner. PMC7824767

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.66mL

2.53mL

1.27mL

25.33mL

5.07mL

2.53mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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