计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,避光,充氩。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Immortalized fibroblasts derived from WT and Pin1 KO mouse embryos Concentration: 1 and 5 μM Incubation Time: 0-8 days Result: Dose-dependently inhibited proliferation of WT fibroblasts, while showed no effect on Pin1 KO fibroblasts. Cell Viability AssayCell Line: MCF10A, HMEC, HeLa, LNCaP, SKOV-3, PANC-1, PC-3, MDA-MB-468 and MDA-MB-231 cells Concentration: 0-10 μM Incubation Time: 48 hours Result: Inhibited normal breast epithelial cells and cancer cells viability even at a low concentration and increased the concentration of PIN1 in MDA-MB-468, SKOV-3, PC-3, LNCaP and PANC-1. Western Blot AnalysisCell Line: Immortalized fibroblasts derived from WT and Pin1 KO mouse embryos and PIN1 KO MDA-MB-231 cells Concentration: 0-10 μM Incubation Time: 48 hours Result: Decreased hyperphosphorylated pRB and Cyclin D1 levels, dose- and time-dependently promoted degradation of PIN1 . Western Blot AnalysisCell Line: MDA-MB-231, MCF10A, MDA-MB-468 and MDA-MB-231 cells Concentration: 0, 2.5 and 5 μM Incubation Time: 48 hours Result: Dose-dependently increased H2AX phosphorylation and caused H2AX phosphorylation in MCF10A, MDA-MB-468 and MDA-MB-231 cell lines. Increased H2AX phosphorylation while other inhibitors such as ATRA, PiB and Juglone disabled to induce H2AX phosphorylation at same concentration. Achieved DNA damage through formation of DNA adducts. RT-PCRCell Line: MDA-MB-231 cells Concentration: 2.5 and 5 μM Incubation Time: 48 hours Result: Dose-dependently inhibitd the activation of mut-p53 and NOTCH1 pathways which are controlled by PIN1. Inhibitd the expression of cFOS HO1, NQO1, TXNRD1 and DNAJAB, and induced cellular responses to oxidative stress.
In Vivo
KPT-6566 (5 mg/kg; i.p. once a day for 26 days) shows no toxicity to mice . MCE 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 6 cells injection Dosage: 5 mg/kg Administration: Intraperitoneal injection; 5 mg/kg once a day; for 26 days Result: Exibited no sign of local or systemic and organ toxicity by post mortem morphologic analyses.
Form:Solid
IC50& Target:IC50: 640 nM (PIN1 PPIase), Ki: 625.2 nM (PIN1 PPIase)
规格
规格或纯度
≥98%
英文名称
KPT-6566
生化机理
KPT-6566 是一种选择性共价脯氨酰异构酶 PIN1 抑制剂，可与 PIN1 的催化位点共价结合，选择性地抑制和降解 PIN1。KPT-6566 对 PIN1 PPIase 结构域的 IC 50 值为 640u2009nM，K i 值为 625.2 nM。
储存条件
2-8°C储存,避光,充氩
运输条件
低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
未知
分子量
443.54
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 19.23 mg/mL (43.36 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于2–8 °C、避光、氩气保护条件下保存。本品在氩气保护下供应，每次取用后请在惰性气体下重新密封。
本产品如何运输？
本产品采用湿冰冷藏运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 881487-77-0，分子式为 C22H21NO5S2，分子量为 443.54 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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