HSD1590-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEHSD1590Cat.No.:HY-126275CASNo.:2379279-96-4分?式:C??H??BN?O?分?量:359.19作?靶點:ROCK作?通路:CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt;TGF-beta/Smad儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(278.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7840mL13.9202mL27.8404mL5mM0.5568mL2.7840mL5.5681mL10mM0.2784mL1.3920mL2.7840mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(17.40mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6.25mg/mL(17.40mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥6.25mg/mL(17.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性HSD1590?種有效的ROCK抑制劑，對ROCK1和ROCK2的IC50值分別為1.22和0.51nM。HSD1590與ROCK結(jié)合的Kd值?于2nM。HSD1590的細胞毒性低。IC50&TargetROCK1ROCK21.22nM(IC50)0.51nM(IC50)體外研究HSD1590(0.5-1μM;24hours)exhibitsanimpressiveattenuationinmigration[1].HSD1590(0.5-10μM;12-24horus)showsthattheexcellentmigrationinhibitionobservedisnotduetocelldeath,butinhibitionoflivecellmigration[1].CellViabilityAssay[1]CellLine:MDA-MB-23cellsConcentration:0.5-10μMIncubationTime:12-24hoursResult:Exhibitedapproximately80%viabilityat12hoursandyieldedanoverallviabilityof63%at24h.REFERENCES[1].DayalN,etal.Potentlyinhibitingcancercellmigrationwithnovel3H-pyrazolo[4,3-f]quinolineboronicacidROCKinhibitors.EurJMedChem.2019Oct15;180:449-456.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400