GlcNAcstatin
目录号 : GC12847
Selective O-GlcNAcase inhibitor
Cas No.:922163-64-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GlcNAcstatin is a highly potent and competitive inhibitor of O-GlcNAcase (OGA) with Ki value of 4.4 nM for human OGA [1].
GlcNAcstatin is a synthetic GlcNAc-configured nagstatin derivative with a larger isobutanamido group on N8 and a phenethyl group on C2. It inhibited bacterial OGA with Ki value of 4.6 pM. For human OGA, GlcNAcstatin also showed a potent inhibition with Ki value of 4.4 nM. Besides that, GlcNAcstatin exerted inhibitory activity against human lysosomal Hex A/B with Ki value of 550 nM, suggesting that it is a selective inhibitor of OGA. In HEK293 cells, treatment of GlcNAcstatin at concentration of 20 nM resulted in increased cellular O-GlcNAc levels of many proteins. GlcNAcstatin also significantly prevented O-GlcNAc from binding to proteins in SH-SY5Y human neuroblastoma cell lysates [1, 2].
References:
[1] Dorfmueller H, Borodkin V, Schimpl M, et al. GlcNAcstatins are nanomolar inhibitors of human O-GlcNAcase inducing cellular hyper-O-GlcNAcylation. Biochem. J, 2009, 420: 221-227.
[2] Dorfmueller H C, Borodkin V S, Schimpl M, et al. GlcNAcstatin: a picomolar, selective O-GlcNAcase inhibitor that modulates intracellular O-glcNAcylation levels. Journal of the American Chemical Society, 2006, 128(51): 16484-16485.
| Cas No. | 922163-64-2 | SDF | |
| Canonical SMILES | CC(C)C(=O)NC1C(C(C(N2C1=NC(=C2)CCC3=CC=CC=C3)CO)O)O | ||
| 分子式 | C20H27N3O4 | 分子量 | 373.45 |
| 溶解度 | Soluble in DMSO | 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 | 2.6777 mL | 13.3887 mL | 26.7773 mL |
| 5 mM | 0.5355 mL | 2.6777 mL | 5.3555 mL |
| 10 mM | 0.2678 mL | 1.3389 mL | 2.6777 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。