KPT-6566
目录号: PL08494 纯度: ≥98.0%
CAS No. :881487-77-0
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中文名称
KPT-6566
英文名称
KPT-6566
英文别名
[((4E)-4-{[(4-tert-butylphenyl)sulfonyl]imino}-1-oxo-1,4-dihydronaphthalen-2-yl)thio]acetic acid;KPT-6566
Cas No.
881487-77-0
分子式
C22H21NO5S2
分子量
443.54
包装储存
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
KPT-6566 是一种选择性的、共价的 prolyl 异构酶 PIN1 的抑制剂,共价结合到 PIN1 的催化位点,选择性地抑制和降解 PIN1。KPT-6566 对 PIN1 PPIase domain 的 IC50 值为 640 nM,Ki 值为 625.2 nM。KPT-6566 可用于癌症的研究。
生物活性
KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC 50 value of 640?nM and a K i value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer.
性状
Solid
IC50 & Target[1][2]
IC50: 640?nM (PIN1 PPIase)
Ki: 625.2 nM (PIN1 PPIase)
体外研究(In Vitro)
KPT-6566 (1-5 μM; 0-8 d) inhibits WT fibroblasts proliferation.
KPT-6566 (0-10 μM; 48 h) inhibits normal breast epithelial cells and cancer cells viability via a PIN1-dependent manner.
KPT-6566 (0-10 μM; 48 h) affects hyperphosphorylated pRB level, Cyclin D1 and PIN1 concentration.
KPT-6566 (2.5-5 μM; 48 h) inhibits the mut-p53, NOTCH1 and NRF2 pathways.
KPT-6566 (0-5 μM; 48 h) induces DNA damage via a PIN1-dependent way. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
KPT-6566 (5 mg/kg; i.p. once a day for 26 days) shows no toxicity to mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week-old female mice with 1 million of MDA-MB-231Luc cells
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Campaner E, et al. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action. Nat Commun. 2017 Jun 9;8:15772.
溶解度数据
In Vitro: DMSO : 19.23 mg/mL (43.36 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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