MS-1020 是一种有效的 ATP 竞争性 JAK3 抑制剂。MS-1020 抑制 JAK3/STAT 信号传导并诱导细胞凋亡 (apoptosis)。MS-1020 促进细胞死亡。MS-1020 降低酪氨酸磷酸化 STAT3 的表达水平。MS-1020 具有研究携带异常 JAK3 信号传导的癌症的潜力。
| 生物活性 | MS-1020 is a potent and ATP-competitiveJAK3inhibitor. MS-1020 inhibits JAK3/STAT signaling and inducesapoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylatedSTAT3levels. MS-1020 has the potential for the research of cancers harboring aberrantJAK3signaling[1]. |
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体外研究
(In Vitro) | MS-1020 (0-50 μM; 24 h) inhibits STAT92E transcriptional activity in cultured Drosophila cells[1].
MS-1020 (0, 10, 30 , 50 μM) decreases the expression of tyrosine phosphorylated STAT3 levels and shows no changes on total STAT3 levels[1].
MS-1020 (0, 10, 30 , 50 μM; 16 h) decreases the expression of IL-2 (100 ng/ml)-induced STAT5 phosphorylation in Nb2 cells[1].
MS-1020 (0, 10, 30 , 50 μM; 72 h) promotes cell death in a time- and dose-dependent manner in L540 cells[1].
MS-1020 (0, 10, 30 , 50 μM; 72 h) induces apoptosis in L540 cells[1].
Western Blot Analysis[1] | Cell Line: | L540, HDLM-2, MDA-MB-468 cells | | Concentration: | 0, 10, 30, 50 μM | | Incubation Time: | | | Result: | Decreased the expression of tyrosine phosphorylated STAT3 levels in a dose-dependent manner and showed no changes on total STAT3 levels. |
Cell Viability Assay[1] | Cell Line: | L540, HDLM-2 cells | | Concentration: | 0, 10, 30, 50 μM | | Incubation Time: | 72 h | | Result: | Promoted cell death in a time- and dose-dependent manner only in L540 cells. |
Apoptosis Analysis[1] | Cell Line: | L540 cells | | Concentration: | 0, 10, 30, 50 μM | | Incubation Time: | 72 h | | Result: | Induced apoptosis in L540 cells and increased the expression of cleavage of Poly (ADP-ribose) polymerase (PARP) and cleaved caspase-3 and cleaved caspase-3, decreased the expression of Bcl-2, Bcl-xL, Mcl-1, and survivin in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
