SIRT2 Inhibitor II (AK-1)
目录号 : GC30922
A SIRT2 inhibitor
Cas No.:330461-64-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | HEK293 cells are co-transfected with 3 μg of pGL2-PGK1-HRE-Luc and 1 μg of pCMV-β-galactosidase plasmids. Twenty-four hours later, the cells are incubated under hypoxic conditions for 24 hr in the presence of 10 μM AK-1 and then lysed with luciferase cell lysis buffer. Luciferase and β-galactosidase activities are measured using luciferin and ο-nitrophenyl-β-d-galactopyranoside, respectively, as substrates. Transfection efficiency is normalized according to β-galactosidase activity[3]. |
References: [1]. 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. | |
AK-1 is a sirtuin 2 (SIRT2) inhibitor (IC50 = 12.5 ?M).1 It induces the formation of α-synuclein aggregates in H4 neuroglioma cells expressing α-synuclein and synphilin-1.2 AK-1 (5 ?M) decreases total cholesterol levels in Neuro2a and primary rat striatal neurons, as well as in hippocampal slice cultures.1 It increases ubiquitination of hypoxia-inducible factor-1α (HIF-1α) in A549 cells and decreases HIF-1α levels in A549, HeLa, HEK293, and HEK293T cells under hypoxic conditions when used at a concentration of 10 ?M.3 AK-1 (1 and 10 ?M in the diet) decreases the loss of rhabdomeres in the ommatidium in the UAS-Httex1p-Q93 transgenic Drosophila model of Huntington's disease.4 Dietary administration of AK-1 (500 and 1,000 ?M) prevents dopaminergic neuronal cell death in the dorsomedial cluster in the elav-GAL4 transgenic Drosophila model of Parkinson's disease.2
1.Taylor, D.M., Balabadra, U., Xiang, Z., et al.A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylaseACS Chem Biol.6(6)540-546(2011) 2.Outeiro, T.F., Kontopoulos, E., Altmann, S.M., et al.Sirtuin 2 inhibitors rescue α-synuclein-mediated toxicity in models of Parkinson's diseaseScience317(5837)516-519(2007) 3.Lee, S.D., Kim, W., Jeong, J.-W., et al.AK-1, a SIRT2 inhibitor, destabilizes HIF-1α and diminishes its transcriptional activity during hypoxiaCancer Lett.373(1)138-145(2016) 4.Luthi-Carter, R., Taylor, D.M., Pallos, J., et al.SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesisProc. Natl. Acad. Sci. USA107(17)7927-7932(2010)
| Cas No. | 330461-64-8 | SDF | |
| Canonical SMILES | O=C(NC1=CC=CC([N+]([O-])=O)=C1)C2=CC=CC(S(=O)(N3CCCCCC3)=O)=C2 | ||
| 分子式 | C19H21N3O5S | 分子量 | 403.45 |
| 溶解度 | DMSO : ≥ 50 mg/mL (123.93 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4786 mL | 12.3931 mL | 24.7862 mL |
| 5 mM | 0.4957 mL | 2.4786 mL | 4.9572 mL |
| 10 mM | 0.2479 mL | 1.2393 mL | 2.4786 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。