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Cellagentech/GSK1210151A (I-BET 151) | BRD2/3/4 inhibitor/C4121-5/5 mg (powder)

ProductDescription

GSK1210151A(I-BET151)isanorally-available,imidazolonoquinoline-basedinhibitoroftheBETfamilyofbromodomains,activeagainstBRD2,BRD3,andBRD4atIC50sof500,250,and800nM,respectively.ItisalsoapotentupregulatorofApoA1withanEC170of100nM.[1]

GSK1210151AwasshowntohaveprofoudnefficacyagainsthumanandmurineMLL-fusionleukemiccelllines,throughtheinductionofearlycellcyclearrestandapoptosis.Themodeofactionispartlyduetotheinhibitionoftranscrdiptionofkeygenes(BCL2,C-MYC,andCDK6)throughthedisplacementofBRD3/4,PAFc,andSECcomponentsthroughchromatin.[2]

BecauseApoA1upregulationisoftenassociatedwithanti-inflammatorypropertiesinnonhepaticcells,GSK1210151Awastestedandshowntoexhibitadose-dependentinhibitionofbothIL-6andTNFaproductioninLPS-stimulatedhumanPBMCs.[3]

Technicalinformation:

ChemicalFormula: C23H21N5O3
CAS#: 1300031-49-5
MolecularWeight: 415.44
Purity: >98%
Appearance: White
ChemicalName: 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one
Solubility: Upto22mMinDMSO
Synonyms: GSK-1210151A,GSK1210151A,I-BET151,I-BET151,1300031-49-5

ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.

Reference:

1.Sealetal.,IdentificationofanovelseriesofBETfamilybromodomaininhibitors:bindingmodeandprofileofI-BET151(GSK1210151A).Bioorg.Med.Chem.Lett.2012,22,2968-2972.PubmedID:22437115
2.Dawsonetal.,InhibitionofBETrecruitmenttochromatinasaneffectivetreatmentforMLL-fusionleukaemia.Nature2011,478,529-533.PubmedID:21964340
3.Mirguetetal.,FromApoA1upregulationtoBETfamilybromodomaininhibition:discoveryofI-BET151.Bioorg.Med.Chem.Lett.2012,22,2963-2967.PubmedID:22386529

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