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57046-73-8

中文名称 (ALPHAZ)-ALPHA-(3-吡啶基亚甲基)-1H-吲哚-3-乙腈
英文名称 Paprotrain
CAS 57046-73-8
分子式 C16H11N3
分子量 245.28
MOL 文件 57046-73-8.mol
57046-73-8 结构式 57046-73-8 结构式

基本信息

中文别名
(ALPHAZ)-ALPHA-(3-吡啶基亚甲基)-1H-吲哚-3-乙腈
英文别名
Paprotrain
2-(1H-Indol-3-yl)-3-pyridin-3-yl-acrylonitrile
(Z)-α-(3-Pyridinylmethylene)-1H-indole-3-acetonitrile
1H-Indole-3-acetonitrile, α-(3-pyridinylmethylene)-, (αZ)-
(alphaZ)-alpha-(3-Pyridinylmethylene)-1H-indole-3-acetonitrile

物理化学性质

熔点202℃
储存条件Sealed in dry,2-8°C
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:6): 0.1 mg/ml; Ethanol: 0.2 mg/ml
形态粉末
颜色Light yellow to yellow
(ALPHAZ)-ALPHA-(3-吡啶基亚甲基)-1H-吲哚-3-乙腈价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/02/08HY-101298(ALPHAZ)-ALPHA-(3-吡啶基亚甲基)-1H-吲哚-3-乙腈
Paprotrain
57046-73-85mg500元
2025/02/08HY-101298(ALPHAZ)-ALPHA-(3-吡啶基亚甲基)-1H-吲哚-3-乙腈
Paprotrain
57046-73-810mM * 1mLin DMSO550元
2025/02/08HY-101298(ALPHAZ)-ALPHA-(3-吡啶基亚甲基)-1H-吲哚-3-乙腈
Paprotrain
57046-73-810mg700元

常见问题列表

生物活性
Paprotrain是可渗透细胞的kinesin MKLP-2 的抑制剂,抑制 MKLP-2 的 ATPase 活性,IC50 值为 1.35 μM,Ki 值为 3.36 μM,同时对 DYRK1A 有中等的抑制作用,IC50值为 5.5 μM。
靶点

MKLP-2

1.35 μM (IC 50 )

体外研究

Paprotrain has been screened on a panel of CNS kinases. While inactive (IC 50 >10 μM) on CDK5 and GSK3, it has shown a moderate activity on DYRK1A (IC 50 =5.5 μM). Time-lapse microscopy shows that disrupting MKlp2 expression with paprotrain results in polar body extrusion failure. This could be rescued after rescuing oocytes from paprotrain in fresh medium. Cell cycle analysis shows that most oocytes are arrested at metaphase I or telophase I. However, oocyte spindle structure and chromosome alignment are not disrupted after the inhibition of MKlp2 by paprotrain. Paprotrain-treated porcine oocytes suffer failure of nuclear maturation. The number of oocytes arrested at early MI stage increase in a dose-dependent manner after KIF20A activity inhibition, while the percentage of oocytes that reach ATI and MII stages decrease after treatment.

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