Bpsbioscience/Romidepsin (FK228, depsipeptide)/27646-1/1 mg
商品编号:
27646-1
品牌:
bpsbioscience
市场价:
¥3900.00
美元价:
2340.00
联系Q Q:
3392242852
电话号码:
4000-520-616
电子邮箱:
info@ebiomall.com
商品介绍
MW:540.7Da
CASRegistry#:128517-07-7
Formula:C24H36N4O6S2
Target:HDAC
Background:
RomidepsinisabicyclicdepsipeptideantibioticisolatedfromthebacteriumChromobacteriumviolaceumwithantineoplasticactivity.Afterintracellularactivation,romidepsinbindstoandinhibitshistonedeacetylase(HDAC),resultinginalterationsingeneexpressionandtheinductionofcelldifferentiation,cellcyclearrest,andapoptosis.Thisagentalsoinhibitshypoxia-inducedangiogenesisanddepletesseveralheatshockprotein90(Hsp90)-dependentoncoproteins.Invitro,romidepsincausestheaccumulationofacetylatedhistones,andinducescellcyclearrestandapoptosisofsomecancercelllineswithIC50valuesinthenanomolarrange.
Description:
Romidepsin,alsoknownasFK228ordepsipeptide,isapotentandselectiveinhibitorofHDAC1andHDAC2,whichareassociatedwiththeregulationofre-expressionofsilencedtumorsuppressorgenes.ItwasthefirstHDACinhibitortomanifestanti-tumoractivityandoriginallyisolatedfromarod-shapedGram-negativebacterium,Chromobacteriumviolaceum,foundinaJapanesesoilsample.RomidepsinexhibitsastrongerinhibitiontowardsHDAC1andHDAC2enzymes(classI),removingacetylgroupsfromthelysineresiduesofN-terminalhistonetailsandmaintainingamoreopenandtranscriptionallyactivechromatinstate,thanHDAC4andHDAC6enzymes(classII).BesidesHDACinhibition,romidepsinisalsoabletoinducecellcyclearrest,cellulardifferentiation,apoptosisandalterationofgeneexpressioninadultmalignancies.
Synonym(s):
Istodax;FK228;FR901228,FK-228;Romidepsin;(1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazABIcyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
Purity:
≥98%byHPLC
BIOLOGicalActivity:
TheIC50forHDAC1is36nMandtheIC50forHDAC2is47nM
Solubility:
SolubleinDMSO
Storage/Stability:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
1.McGrawAL.AmJHealthSystPharm.2013Jul1;70(13):1115-22.
2.KimM,etal.AnnPharmacother.2012Oct;46(10):1340-8.
3.HorwitzSM.ClinAdvHematolOncol.2012May;10(5):333-4.
4.VanderMolen,KM,etal.J.Antibiotics2011:64,525-531.
2.KimM,etal.AnnPharmacother.2012Oct;46(10):1340-8.
3.HorwitzSM.ClinAdvHematolOncol.2012May;10(5):333-4.
4.VanderMolen,KM,etal.J.Antibiotics2011:64,525-531.
ScientificCategory:
DeacetylaseInhibitor
ProductType:
Inhibitor
Datashownislot-specific.Contactusforspecificinformationonotherlots.
品牌介绍
bpsbioscience简介:为生命科学研究提供ELISA试剂盒(仅供科研)、抗体和抗原(仅供科研)、流式抗体,使您的检测结果更稳定可靠,用心服务科研。我公司国内总代理,华东地区代理bpsbioscience 专业经营进口胎牛血清、细胞因子、ELISA试剂盒、细胞、抗体、生物试剂、耗材、培养基、一抗、二抗、其产品吸附均匀,吸附性好,空白值低,孔底透明度高,代做ELISA实验等。