RU-SKI 43 HCL;HHAT INHIBITOR
RU-SKI 43 HCL;HHAT INHIBITOR 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMF：30 mg/ml； DMSO：30 mg/ml；乙醇：30 mg/ml；乙醇:PBS(pH 7.2) (1:1): 0.5 mg/ml |
| 形态 | 结晶固体 |
| 颜色 | 白色至米白色 |
RU-SKI 43 HCL;HHAT INHIBITOR 用途与合成方法
IC50: 850 nM (Hhat)
RU-SKI 43 hydrochloride (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells.
RU-SKI 43 hydrochloride (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours.
RU-SKI 43 hydrochloride (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells.
RU-SKI 43 hydrochloride (10 μM; 48 hours) results in decreased phosphorylation (47-67%) of four proteins in the Akt pathway, including Akt (phosphorylation at both Thr307 and Ser473), PRAS40, Bad and GSK-3β. RU-SKI 43 treatment also decreases phosphorylation of mTOR and S6, members of the mTOR signaling pathway.
RU-SKI 43 hydrochloride behaves as an uncompetitive inhibitor (K
i
=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (K
i
=6.9 μM) with respect to
125
I-iodo-palmitoylCoA.
Cell Proliferation Assay
| Cell Line: | AsPC-1 and Panc-1 pancreatic cancer cells |
| Concentration: | 10 μM |
| Incubation Time: | For 6 days (drugs were replenished every 48 hours) |
| Result: | Strongly decreased cell proliferation (83% in AsPC-1 cells). |
Western Blot Analysis
| Cell Line: | COS-1 cells expressing HA-Hhat and Shh |
| Concentration: | 10 or 20 μM |
| Incubation Time: | 5 hours |
| Result: | Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours. |
RU-SKI 43 hydrochloride has a t
1/2
of 17 min in mouse plasma after IV administration.
