反应生物学/CUDC-101/EI-HDC-010
商品编号:
EI-HDC-010
品牌:
reactionbiology
市场价:
¥3000.00
美元价:
1800.00
产品分类:
反应底物
公司分类:
Reaction_substrate
联系Q Q:
3392242852
电话号码:
4000-520-616
电子邮箱:
info@ebiomall.com
商品介绍
CUDC-101
7-((4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)oxy)-N-hydroxyheptanamide
CUDC-101 is a novel hybrid dual-acting HDAC and receptor tyrosine kinase inhibitor. Itis a potent HDAC inhibitor which also inhibits EGFR and HER2, IC50 = 4.4, 2.4 and 15.7 nMrespectively. It not only blocks EGFR and HER2 but also attenuatesmultiple compensatory pathways such as AKT, HER3 and MET which enable tumorcells to escape the effects of conventional EGFR/HER2 inhibitorsPhysical Properties: White to off-whitepowderMW = 434.5 C24H26N4O4
Analysis: >99% (HPLC); NMR(Conforms); MP=188-190oC
Solubilization: May be dissolved in DMSO (25 mg/ml)
Storage: Store desiccated assupplied at -20°C for up to 2 years. Store solutions at -20°C for up to 1 month.
Amount: 5mg品牌介绍
Reaction Biology描述:
人类重组EZH2incomplexwithhumanrecombinantsEED.TotalcomplexMWis228.7kDa.Allproteinsarefull长度(residue2throughC末端)也是全美-expressedinaninsectcell / baculovirusexpressionsystem.TheEEDsubunitincorporatesanN-terminalStrepandFlag-tagandallothersincludeanN-terminalHis-tag.CatalyzesthetransferofmethylgroupsfromS腺苷-L-甲硫氨酸(SAM)tothee-aminofunctionofproteinL-lysineresidues,specificallylysine-27ofhistoneH3( H3K27)。在开发过程中,Polycomb Repressive Complex 2(PRC2)是主要的甲基转移酶对IBL的反应eforgeneratingtrimethylatedhistoneH3lysine-27(的H3K27me3),anepigeneticmarkessentialforprogrammedrepressionofgeneexpression1-5.EZH2,whichincludesaSETmethyltransferasedomain,isthecatalyticsubunitofPRC21,6.ThecoreofthecatalyticcomplexincludesEZH2,EED,SUZ12andRbAp48,whileadditionofAEBP2significantlyenhancesthemethyltransferaseactivityofthecomplex(> 3×)6.EZH2isoverexpressedinawiderangeofhumancancersanditsoverexpressioncancorrelatewithtumorprogression,increasedmetastasisandpoorprognosis(seereview7).DepletionofEZH2and / orotherPRC2componentscaninhibitgrowthorinduceapoptosisincancercells6,8-10.Consequently,EZH2isconsideredapromisingtargetforthedevelopmentofanti -癌症疗法11
存取编号: EZH2NM_001203247,EEDNM_003797,SUZ12NM_015355
包括酰胺酸:EZH22-746,EED2-441,SUZ122-739
标记(S):EEDhasanN末端链霉菌标记标签,其他所有N末端His标签
分子量:228.7kDa
EXPRESSIONSYSTEM :昆虫细胞/杆状病毒
SUPPLIEDAS:Solutionofpurifiedrecombinantproteinin20mMTris盐酸,pH8,150mMNaCl,2mMMgCl 2,2mMDTT,20%甘油(w / v),0.01%NP-40asdeterminedbyOD 280。
储存:-70°C。在使用前应迅速融化并储存。应保留未使用的未稀释蛋白质,例如干燥/冰乙醇液中的氮。尽可能减少冻融/解冻,但不建议使用稀释体积太小(<5µl)的稀释蛋白质。
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