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RU-SKI 43
CAS No. 1043797-53-0
RU-SKI 43 ( RUSKI-43 )
产品货号. M10217 CAS No. 1043797-53-0
Hhat（Hedgehog 酰基转移酶）的小分子抑制剂，IC50 为 0.85 uM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥867 | 有现货 |
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| 10MG | ￥1264 | 有现货 |
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| 25MG | ￥2725 | 有现货 |
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| 50MG | ￥4027 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥808 | 有现货 |
|
生物学信息
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产品名称RU-SKI 43
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述Hhat（Hedgehog 酰基转移酶）的小分子抑制剂，IC50 为 0.85 uM。
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产品描述A small molecule inhibitor of Hhat (Hedgehog acyltransferase) with IC50 of 0.85 uM; specific to Shh palmitoylation and no effect for palmitoylation of H-Ras, Fyn and myristoylation of c-Src; reduces pancreatic cancer cell proliferation and Gli-1 activation through Smoothened-independent non-canonical signaling, inhibits two key proliferative pathways regulated by Akt and mTOR.
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体外实验RU-SKI 43 (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells. RU-SKI 43 (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours. RU-SKI 43 (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells. RU-SKI 43 (10μM; 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 behaves as an uncompetitive inhibitor (Ki=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9 μM) with respect to 125I-iodo-palmitoylCoA. They are for reference only.RU-SKI 43 :Cell Proliferation AssayCell 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).
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体内实验RU-SKI 43 has a t1/2 of 17 min in mouse plasma after IV administration.
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同义词RUSKI-43
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通路GPCR/G Protein
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靶点Hedgehog (Hh)
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受体Hedgehog (Hh)
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研究领域Cancer
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适应症——
化学信息
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CAS Number1043797-53-0
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分子量386.5508
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分子式C22H30N2O2S
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCCC(C)CNCC(=O)N1CCC2=C(C1COC3=CC=CC(=C3)C)C=CS2
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化学全称Ethanone, 1-[6,7-dihydro-4-[(3-methylphenoxy)methyl]thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-methylbutyl)amino]-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Petrova E, et al. Nat Chem Biol. 2013 Apr;9(4):247-9.
2. Petrova E, et al. Oncogene. 2015 Jan 8;34(2):263-8.
3. Matevossian A, et al. Mol Cancer. 2015 Apr 1;14:72.
