ProductDescription
KU55933isanATP-competitive,thioanthrene-pyranone-basedinhibitorofATMkinasewithanIC50of13nMandKiof2.2nMand>100-foldselectivityoverPI3Krelatedkinases.[1]KU55933inhibitscellproliferationbyinducingG1cellcyclearrestbydownregulationofcyclinD1synthesisinMDA-MB-453breastcancercellsandPC-3prostatecancercells.[2]KU55933inhibitsinsulin-andIGF1-stimulatedAktphosphorylationatbothSer473andThr308.[2]ATMcellularinhibitionbyKU55933wasdemonstratedinadditionalphosphorylationtargets,includingp53Ser15,H2AXSer139,NBS1Ser343,Chk1Ser345,andSMC1Ser966.[1]
KU55933isbeingstudiedasarADIosensitizer,havingbeenshowntosensitizeHeLacellstotheeffectsoftopoisomeraseinhibitors,etoposide,doxorubicin,amsacrine,andcamptothecin.[1]Whenincombinationwithrapamycin,KU55933inducesapoptosisandarrestsanyinducedfeedbackactivationofAkt.[2]
Technicalinformation:
ChemicalFormula: | C21H17NO3S2 | |
CAS#: | 587871-26-9 | |
MolecularWeight: | 395.49 | |
Purity: | >98% | |
Appearance: | White | |
ChemicalName: | 2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one | |
Solubility: | Upto100mMinDMSO | |
Synonyms: | KU-55933,KU55933,KU55933 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | Hicksonetal.,Identificationandcharacterizationofanovelandspecificinhibitoroftheataxia-telangiectasiamutatedkinaseATM.CancerRes.2004,64(24),9152-9159.PubmedID:15604286 |
2. | Lietal.,TheATMinhibitorKU-55933suppressescellproliferationandinducesapoptosisbyblockingAktincancercellswithoveractivatedAkt.Mol.Cancer.Ther.2010,9(1),113-125.PubmedID:20053781 |
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