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Rhosin (G04; G-04) HCl, the hydrochloride salt of Rhosin, is a novel and potent Rho GTPase inhibitor. It inhibits WT RhoA with an affinity ~0.4 uM. Rho GTPases have been implicated in diverse cellular functions and are potential therapeutic targets.
| ln Vitro |
Mammospheres produced from MCF7 cells exhibit dose-dependent reductions in RhoA and p-MLC1 activity, with an EC50 of ~30-50 μM. Additionally, mammosphere size and number in MCF7 cells are reduced [1].
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| ln Vivo |
The therapy of Russell (40 mg/kg; i.p.) inhibits social avoidance brought on by stress related to social defeat. In C57Bl6/J (Jackson) mice, Russell also prevents the sucrose preference deficit caused by failure [3]. ?Stress-induced social avoidance is lessened when Russell (30 μM; bilateral intranuclear accumbens (NAc) infusion) is used. In medium spiny neurons with the NAc dopamine 1 receptor, rosin inhibits the hyperexcitability brought on by stress (D1-MSN). Russell stops the excitatory transmission on NAc D1-MSNs from decreasing. In mice that fail, rosin increases spine density [3].
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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: Russell 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. |
| References |
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| Molecular Formula |
C20H19CLN6O
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|---|---|
| Molecular Weight |
394.8575
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| Exact Mass |
394.13
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| Elemental Analysis |
C, 60.84; H, 4.85; Cl, 8.98; N, 21.28; O, 4.05
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| CAS # |
1281870-42-5
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| Related CAS # |
Rhosin;1173671-63-0
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| PubChem CID |
52998412
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
541
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| Defined Atom Stereocenter Count |
1
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| SMILES |
Cl[H].O=C([C@@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])[H])N([H])/N=C(/[H])\C1C([H])=C([H])C2C(C=1[H])=NC([H])=C([H])N=2
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| InChi Key |
SFRGBDFQSLZYLF-GRYLRVQNSA-N
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| InChi Code |
InChI=1S/C20H18N6O.ClH/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);1H/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;hydrochloride
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| Synonyms |
Rhosin hydrochloride; Rhosin HCl; 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~126.63 mM)
H2O : ~16.67 mg/mL (~42.22 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (6.33 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5325 mL | 12.6627 mL | 25.3254 mL | |
| 5 mM | 0.5065 mL | 2.5325 mL | 5.0651 mL | |
| 10 mM | 0.2533 mL | 1.2663 mL | 2.5325 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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