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主营:激酶、磷酸二酯酶、磷酸酶、组蛋白去甲基化酶、组蛋白甲基化转移酶、HDACs、聚ADP核糖聚合酶
℡ 4000-520-616
℡ 4000-520-616
Bpsbioscience/GSK J4 HCl/27627-1/10 mg
产品编号:27627-1
市  场 价:¥3500.00
场      地:美国(厂家直采)
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$175.00
品      牌: BPS Bioscience
公      司:BPS Bioscience Inc.
公司分类:
Bpsbioscience/GSK J4 HCl/27627-1/10 mg
商品介绍
MW:454Da
CASRegistry#:1373423-53-0
Formula:C24H27N5O2•HCl
Target:JMJD3,UTX
Background:
GSKJ4isapotentcell-permeableinhibitorofthehistoneH3lysine27(H3K27)demethylaseJMJD3.GSKJ4isanethylesterderivativeofGSKJ1,aJMJD3inhibitor(IC50=60nM)withrestrictedcellularpermeABIlityduetothehighlypolarcarboxylategroup,andrapidlyhydrolyzedbymacrophageesteraseuponadmiNISTrationleADIngtothegenerationofpharmacologicallyrelevantintracellularconcentrationofGSK-J1.GSKJ4hasbeenfoundtodose-dependentlyinhibittheproductionoftumor-necrosisfactor-α(TNF-α),aLPS-drivencytokineinvolvedinvariousfnflammatorydisorders(IC50=9µM).
Description:
GSKJ4HClisacellpermeableprodrugofGSKJ1,whichisthefirstselectiveinhibitoroftheH3K27histonedemethylaseJMJD3andUTXwithIC50of60nMandinactiveagainstapanelofdemethylasesoftheJMJfamily.
Synonym(s):
ethyl3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
Purity:

≥98%byHPLC

BIOLOGicalActivity:
InhibitsJMJD3andUTXwithIC50of60nMandinactiveagainstapanelofdemethylasesoftheJMJfamily(IC50value>50µM).
Solubility:
SolubleinDMSO84mg/ml,water84mg/ml,ethanol84mg/ml
Storage/Stability:

Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.

Reference(s):
KruidenierL,etal.Nature.2012Aug16;488(7411):404-8.
ScientificCategory:
DemethylaseInhibitor
ProductType:
Inhibitor
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品牌介绍

BPS bioscience总部坐落于世界最大之一的美国圣地亚哥生命科学研究机构和公司集中地的中心。公司主要提供激酶、磷酸二酯酶、磷酸酶、组蛋白去甲基化酶、组蛋白甲基化转移酶、HDACs、聚ADP核糖聚合酶。BPS公司为药物研发用重组酶类的提供了最大选择之一。产品类型 重组酶类;分子细胞生物学;重组蛋白;分析试剂盒;底物;重组细胞系

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