| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S84954-10mg促销 |
98% | ￥450.00 ￥350.00 |
10 | - | - | - | - |
|
S84954-25mg促销 |
98% | ￥1060.00 ￥850.00 |
9 | - | - | - | - |
|
S84954-50mg促销 |
98% | ￥1850.00 ￥1480.00 |
7 | - | - | - | - |
|
S84954-100mg促销 |
98% | ￥3330.00 ￥2660.00 |
2 | - | - | - | - |
|
S84954-250mg促销 |
98% | ￥7410.00 ￥5930.00 |
2 | - | - | - | - |
|
| 产品描述： | AK-1是一种有效的，特异性的和细胞可渗透的SIRT2抑制剂，其 IC50 值为 12.5 μM。 |
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| 靶点： | SIRT2:12.5 μM (IC50);Sirtuin | ||||||||||||||||||||
| 体外研究： | AK-1 achieves significant neuroprotection in Huntington’s disease flies at 10 μM, improving the number of rhabdomeres from 5.2 to 5.6. AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50 of 12.5 μM. AK-1 treatment induces proteasomal degradation of the Snail transcription factor through inactivation of the NF-κB/CSN2 pathway. Reduction in the level of Snail results in upregulation of p21, leading to G1 arrest, slow proliferation, and slow wound-healing activity. The regulation of Snail-p21 axis by AK-1 also occurs in HT-29 colon cancer cells. Under hypoxic conditions, AK-1 increases the ubiquitination of HIF-1α in a VHL-dependent manner, leading to the degradation of HIF-1α via a proteasomal pathway. Downregulation of HIF-1α expression reduces its transcriptional activity and, eventually, reduces the expression of BNIP3, one of HIF-1 target genes, in AK-1-treated cells. | ||||||||||||||||||||
| 参考文献： | 1. Ruth Luthi-Carter, et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc Natl Acad Sci U S A. 2010 Apr 27;107(17):7927-32. 2. Lee SD, et al. AK-1, a SIRT2 inhibitor, destabilizes HIF-1α and diminishes its transcriptional activity during hypoxia. Cancer Lett. 2016 Apr 1;373(1):138-45. 3. Luthi-Carter R, et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc Natl Acad Sci U S A. 2010 Apr 27;107(17):7927-32. 4. David M. Taylor, et al. A Brain-Permeable Small Molecule Reduces Neuronal Cholesterol by Inhibiting Activity of Sirtuin 2 Deacetylase. ACS Chem Biol. 2011 Jun 17;6(6):540-6. 5. Cheon MG, et al. AK-1, a specific SIRT2 inhibitor, induces cell cycle arrest by downregulating Snail in HCT116 human colon carcinoma cells. Cancer Lett. 2015 Jan 28;356(2 Pt B):637-45. |
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| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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