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| 10mg |
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| Other Sizes |
| Targets |
Rhosin targets the RhoA GTPase by binding to the Rho GEF binding domain. It specifically binds to RhoA with a Kd of 354 nM and prevents RhoA from interacting with its guanine nucleotide exchange factors (GEFs). The compound shows selectivity for RhoA over Cdc42, Rac1, and the GEF LARG.
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| ln Vitro |
The RhoA and p-MLC1 activity of MCF7 cell-derived microspheres are dose-dependently decreased by rhosin (EC50 ~30-50 μM), which also causes a decrease in the size and quantity of microspheres in MCF7 cells [1].
In vitro, rhosin specifically binds to RhoA with a Kd of approximately 0.4 μM (354 nM). It inhibits RhoA-GEF interaction without affecting Cdc42 or Rac1, nor the GEF LARG. The compound induces apoptosis in cancer cell lines through RhoA pathway inhibition. |
| ln Vivo |
Social avoidance brought on by social defeat stress is avoided with Russell (40 mg/kg; i.p.) treatment. Russell also prevents the C57Bl6/J (Jackson) mice from developing the failure-induced sucrose preference deficit [1]. Social avoidance brought on by stress is lessened by Russell (30 µM; bilateral intranuclear accumbens (NAc) injection). In NAc dopamine 1 receptor medium spiny neurons, rosin inhibits the hyperexcitability brought on by stress (D1-MSN). Russell stops NAc D1-MSNs from experiencing a decrease in excitatory transmission. Spine density is increased in failing mice by rosin [1].
In vivo activity data for rhosin are limited. As a RhoA inhibitor, it would be expected to show antitumor activity in animal models of cancer. Specific in vivo efficacy data are not available in the published literature. The compound is primarily used as a research tool for studying Rho GTPase signaling. |
| Enzyme Assay |
In vitro RhoA binding assays measure rhosin's affinity for RhoA. Purified RhoA protein or cell lysates are incubated with varying concentrations of the compound. Binding affinity (Kd) is determined by surface plasmon resonance or fluorescence-based methods. Selectivity against Cdc42 and Rac1 is assessed in parallel assays.
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| Cell Assay |
In vitro cell-based assays evaluate rhosin in cancer cell lines. Cells are treated with varying concentrations, and RhoA activity is measured by pull-down assays for active RhoA-GTP. Apoptosis is assessed by annexin V staining or caspase activation. Cell proliferation is measured by MTT assays.
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| Animal Protocol |
Animal/Disease Models: D1-GFP or D2-GFP hemizygous mice on C57BL/6J background [3]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Rhosin was administered systemically 15 minutes before failure to block RhoA activation. While failure Dramatically diminished the amount of time experimental mice spent interacting with new mice, giving Russell suppressed this effect without affecting motor behavior. In vivo animal studies for rhosin would follow standard protocols for anticancer agents. Tumor-bearing mice would be administered the compound via appropriate routes. Tumor growth inhibition, apoptosis markers, and survival would be measured. Specific study designs are not detailed in the available literature. |
| References |
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| Additional Infomation |
Rhosin is a D-tryptophan derivative formed by the condensation of the carboxyl group of D-tryptophan with the amino group of (quinoxalo-6-yl)methylenehydrazine. It directly targets the Rho GEF binding domain, thereby preventing Rho from interacting with its GEF. It exhibits activity as a RhoA inhibitor, RhoC inhibitor, and antitumor drug. It is a D-tryptophan derivative, a quinoxalo-line derivative, and a hydrazone compound.
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| Molecular Formula |
C22H22N4O
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|---|---|
| Molecular Weight |
358.44
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| Exact Mass |
358.154
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| CAS # |
1173671-63-0
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| Related CAS # |
Rhosin hydrochloride;1281870-42-5
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| PubChem CID |
9552914
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| Appearance |
Light yellow to brown solid
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.726
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| LogP |
2.45
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
541
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4
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| InChi Key |
FGYHLIHEFHCMPP-FVWOBLMASA-N
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| InChi Code |
InChI=1S/C20H18N6O/c21-16(10-14-12-24-17-4-2-1-3-15(14)17)20(27)26-25-11-13-5-6-18-19(9-13)23-8-7-22-18/h1-9,11-12,16,24H,10,21H2,(H,26,27)/b25-11+/t16-/m1/s1
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| Chemical Name |
(2R)-2-amino-3-(1H-indol-3-yl)-N-[(E)-quinoxalin-6-ylmethylideneamino]propanamide
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| Synonyms |
Rhosin G-04 G04
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~139.5 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7899 mL | 13.9493 mL | 27.8987 mL | |
| 5 mM | 0.5580 mL | 2.7899 mL | 5.5797 mL | |
| 10 mM | 0.2790 mL | 1.3949 mL | 2.7899 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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