Source | M.W. | 396.4 | CAS No. | 1243244-14-5 | |
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Structural Info | |||||
Formulation | Powder | ||||
Reconstitution | Before reconstitution, werecommend a brief spin to drive down any material dislodged from the bottom ofthe tube. The compound is soluble inDMSO. | ||||
Stability | The powder is stable for atleast 2 year if stored at -20 °C. The dissolved compound is stable for at least 1 month at 4 °C, butshould be stored in aliquots at -20 °C for longer term. Protect from light. | ||||
Purity | Greater than 99% as determined by LC/MS analysis. | ||||
Biological Activity | In a co-culture assay measuring the activation of the TCF reporter gene by Wnt3a-secreting cells, this compound gives IC50 of 0.2 to 0.6 nM. | ||||
Country of Origin | USA |
LGK974 isa potent and specific inhibitor of O-acyltransferase Porcupine (Porcn)that acylates Wnt proteins required for their biological activities. The structure of LGK974 was recentlypublished (Ref. 1). Not only morepotent than the IWP1,2,3,4 Porcn inhibitors (Ref. 2), LGK974 is also suitablefor in vivo studies and is currentlyin the Phase I clinical trials to treat cancers.Ref 1. Discovery of LGK974: Aselective Porcupine inhibitor targeting Wnt signaling in cancer. Shifeng Pan(Novartis), 2013 AACR Annual Meeting.Ref2. Chen B., et al. Smallmolecule-mediated disruption of Wnt-dependent signaling in tissue regenerationand cancer. Nat Chem Biol. 2009;5(2):100-7.
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2、可逆抑制剂:包括
a、竞争性抑制剂,抑制剂与底物竞争性结合酶反应中心,使Km增大,而Vmax不变 b、非竞争性抑制剂,酶与抑制剂结合后还能与底物结合,但活性降低,使Vmax减小,而Km不变
c、反竞争性抑制剂,酶只能与底物结合后才能与抑制剂结合,Vmax与Km都减小
可逆抑制剂可用透析等方法除去,使酶恢复作用
1.对于抑制剂筛选工作(求ic50)是不是体系内酶与底物的量(底物应该是过量的)对实验结果影响不大。
2.如果要求算Km值,是不是需要知道反应产物的绝对量。反应时间文献上都是5分钟,反应速度就用反应产物量除以反应时间即可。
3.酶是进口分装的,规格5U,一次用不完,用PBS稀释后如何保存
谢谢
1、测定酶比活力:底物需要过量么?测定时间多长?是否可以加入过量的底物,然后测定3min吸光度的增加值,从吸光度的变化值计算比活力。
2、在酶抑制剂筛选的过程中,是否需要保证底物过量?还是要水浴一定时间让反应完全?我看到文献说用终浓度为0.1μmol/mL的底物,终浓度为45U/ml的酶,我想问,假设总体积为1ml,那么终浓度为45U/ml的酶岂不是每分钟能转化4.8μmol的底物?那么0.1μmol/mL的底物不就几秒钟就反应完了?那么怎么测定初速度?
《血管紧张素转换酶抑制剂在心血管病中应用的中国专家共识》.PDF(242.69k)
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