Protein kinase D inhibitor 1 (compound 17m) 是一种有效的泛PKD抑制剂，IC50为 17~35 nM。Protein kinase D inhibitor 1 可抑制 PKD 依赖性的皮质激素磷酸化。
| 生物活性 | Protein kinase D inhibitor 1 (compound 17m) is a pan-PKDinhibitor, withIC50values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation[1]. |
| IC50& Target | PKD3 17 ± 8 nM (IC50) | PKD2 35 ± 5 nM (IC50) | PKD1 35 ± 10 nM (IC50) |
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体外研究
(In Vitro) | Protein kinase D inhibitor 1 (compound 17m) displays excellent PKD2 inhibition with almost no remaining kinase activity at 1 μM[1].
Protein kinase D inhibitor 1 displays only weak antiproliferative activity, and does not significantly affect PANC-1 cell proliferation at a concentration of 5 μM[1].
Protein kinase D inhibitor 1 (0-100 μM, 72 h) shows antitumor activity[1].
Cell Viability Assay[1] | Cell Line: | LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, K-562 | | Concentration: | 0-100 μM | | Incubation Time: | 72 h | | Result: | Inhibited of tumor cell growth of LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, and K-562, with IC50values of 80.6 ± 7, 40.7 ± 14.5, 42.7 ± 4.9, 17.9 ± 4.1, 35.3 ± 10.4, >95.8, >100, and >100, respectively. |
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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. |
