T35616
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Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mammary carcinoma cells in a chamber cell migration assay (IC50= 29 μM).2It enhances cytotoxicity induced by vinblastine in vincristine-resistant P388/VCR cells.3 |
T83805
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Rp-Adenosine-5'-O-(1-thiodiphosphate)(Rp-ADP-α-S)是ADP-α-S的含硫异构体,是磷酸化酶激酶的抑制剂(Ki = 0.53 µM)。此化合物能诱导分离的人类血小板聚集(EC50 = 20 µM),并能引发经卡巴胆碱预收缩的豚鼠乙状结肠松弛(EC50 = 58.9 µM)。 |
T83806
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Sp-Adenosine-5’-O-(1-thiodiphosphate) (Sp-ADP-α-S) 是硫含量核苷酸衍生物ADP-α-S的一种异构体。它是磷酸化酶激酶的抑制剂(Ki = 0.53 µM)。Sp-ADP-α-S能引起人类孤立血小板聚集(EC50 = 20 µM),并能使羧胺胆碱预收缩的豚鼠taenia coli松弛(EC50 = 58.9 µM)。 |
T83808
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Sp-Adenosine-5'-O-(1-thiotriphosphate) (Sp-ATP-α-S) 是一种含硫核苷酸衍生物 ATP-α-S 的异构体,也是嘌呤P2Y1受体的激动剂。在表达P2Y1受体的HEK293细胞中增加钙离子的流动(对人类受体的EC50 = 9.4 nM)。Sp-ATP-α-S 抑制了ADP诱导的孤立人类血小板聚集(Ki = 4 μM)。它还能引起经卡巴胆碱预收缩的豚鼠十二指肠松弛(EC50 = 426 nM)。 |
T83807
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Rp-Adenosine-5'-O-(1-thiotriphosphate)(Rp-ATP-α-S)是一种含硫核苷酸衍生物ATP-α-S的异构体,同时也是嘌呤P2Y1受体的激动剂。在表达人类P2Y1受体的HEK293细胞中,Rp-ATP-α-S能增加钙的动员(EC50 = 75 nM)。该化合物与洗涤的人类孤立血小板结合(Ki = 156 nM),抑制由ADP引发的人类富血小板血浆(PRP)的聚集(pA2 = 4.74),并且能够抑制前列腺素E1(PGE1)在人类孤立PRP中引发的cAMP产生(pA2 = 5.26)。同时,Rp-ATP-α-S还能引起用氨基甲酰胆碱预先缩紧的豚鼠结肠条带的松弛(EC50 = 56 nM)。此外,Rp-ATP-α-S已经被用于合成被细菌核糖开关识别的环状二核苷酸。 |