CRT0066854
目录号: PL09898 纯度: ≥99%
CAS No. :1438881-19-6
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中文名称
CRT0066854
中文别名
(2S)-3-苯基-n1-[5,6,7,8-四氢-2-(4-吡啶)[1]苯并噻吩并[2,3-d]嘧啶-4-基]-1,2-丙二胺
英文名称
CRT0066854
英文别名
(2S)-3-Phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine;(2S)-3-Phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propane;CRT0066854
Cas No.
1438881-19-6
分子式
C24H25N5S
分子量
415.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
CRT0066854 是一种强效选择性非典型 PKC 同工酶抑制剂。CRT0066854 抑制 PKCι,PKCζ 和 ROCK-II 的 IC50 的值分别为 132nM,639 nM 和 620 nM。
生物活性
CRT0066854 is a potent and selective atypical PKC isoenzymes inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC 50 values of 132 nM, 639 nM, and 620 nM, respectively.
性状
Solid
IC50 & Target[1][2]
PKCζ 639 nM (IC50) ROCK2 620 nM (IC50
体外研究(In Vitro)
CRT0066854 displaces a crucial Asn-Phe-Asp motif that is part of the adenosine-binding pocket and engages an acidic patch used by arginine-rich PKC substrates.
CRT0066854 (0.2-1.2 μM; 6 days) is able to restore polarized morphogenesis in the dysplastic H-Ras spheroids, and the maximal proportion of spheroids with PSALs is at the lower dose of 1.2 μM.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Kj?r S, et al. Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes. Biochem J. 2013 Apr 15;451(2):329-42.
溶解度数据
In Vitro: DMSO : 50 mg/mL (120.32 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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