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

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEChaetocinCat.No.:HY-N2019CASNo.:28097-03-2分?式:C??H??N?O?S?分?量:696.84作?靶點(diǎn):HistoneMethyltransferase;Bacterial;Antibiotic作?通路:Epigenetics;Anti-infection儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥26mg/mL(37.31mM)掃描?維碼，H2O:<0.1mg/mL(insoluble)運(yùn)?溶解?案計(jì)算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4350mL7.1752mL14.3505mL5mM0.2870mL1.4350mL2.8701mL10mM0.1435mL0.7175mL1.4350mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:2.08mg/mL(2.98mM);Suspendedsolution;Needultrasonic此?案可獲得2.08mg/mL(2.98mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述1/3www.MedChemEwww.MedChemE2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.08mg/mL(2.98mM);Clearsolution此?案可獲得≥2.08mg/mL(2.98mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Chaetocin組蛋?甲轉(zhuǎn)移酶(HMT)SU(VAR)3-9的特異性抑制劑，IC50值為0.6μM。Chaetocin也可抑制硫氧還蛋?還原酶(TrxR)，IC50值為4μM。IC50&TargetIC50:0.6μM(HMT)[1],4μM(TrxR)[2]體外研究Chaetocinisinitiallyisolatedfromthefermentationbrothofchaetomiumminutumandbelongstotheclassof3-6epidithio-diketopiperazines(ETPs).TheIC50forSU(VAR)3-9is0.6μMandactsasacompetitiveinhibitorforS-adenosylmethionine.ChaetocininhibitsthehumanorthologofdSU(VAR)3-9withasimilarIC50valueof0.8μM.ItinhibitsotherknownLys9-specificHMTssuchasmouseG9aandNeurosporacrassaDIM5withahigherIC50valuesof2.5and3mM,respectively[1].ChaetocininhibitsTrxR1-initiatedturnoverofthesyntheticsubstrateDTNBinacell-freeassayinadose-responsivemannerwithanIC50ofabout4μM[2].體內(nèi)研究SL-2Drosophilatissuecellsareculturedinthepresenceorabsenceoftheinhibitor.Chaetocinhasatoxiceffectoncellsgrowninculture.Toxicityishighlydependentontheinitialcelldensitywhenchaetocinisaddedtotheculture.ThenumberofH3moleculesdimethylatedatLys9(H3K9me2)ismarkedlyreducedwhencellsaregrowninmediumcontaining0.5μMchaetocinafter5d.Histonesisolatedfromcellstreatedwith0.1μMandforashortertimealsoshowsadropinLys9methylation,butnotasstronglyaswiththehigherconcentration[1].PROTOCOLCellAssay[2]HeLacellsaretransfectedwith1μgpcDNAorpcDNA-Trx.TwentyfourhaftertransfectionthecellsaretreatedwitheitherDMSO,100nMchaetocinor100nMdoxorubicinfor24h.Thecellsarethentrypsinizedandmanuallycountedintrypanbluetoexcludedeadcells.Forimmunoblotting(24haftertransfections),cellsaretrypsinized,ishedincoldPBS,andlysedinCelLyticlysisbuffercontainingproteaseinhibitors.ProteinisanalyzedbyBCAassayandlysatesareelectrophoresedon15%SDSgelsandtransferredtonitrocellulose.Immunoblottingforthioredoxinandactinisthenperformed[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].GreinerD,etal.IdentificationofaspecificinhibitorofthehistonemethyltransferaseSU(VAR)3-9.NatChemBiol.2005Aug;1(3):143-5.[2].TibodeauJD,etal.Theanticanceragentchaetocinisacompetitivesubstrateandinhibitorofthioredoxinreductase.AntioxidRedoxSignal.2009May;11(5):1097-106.2/3www.MedChemEwww.MedChemEMcePdfHeight關(guān)注MCE中國公眾號(hào)，

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