1782573-67-4
1782573-67-4 结构式
基本信息
HHAT INHIBITOR
2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride
物理化学性质
常见问题列表
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.