STK393606
目录号 : GC12204
A selective inhibitor of 15-PGDH
Cas No.:355827-05-3
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
Target: NAD+-dependent type-I 15-hydroxy PGDH
IC50: 26.4 nM
Ki: 5 nM
STK393606 is a competitive inhibitor of NAD+-dependent type-I 15-hydroxy PGDH, with the IC50 value of 26.4±2.4 nM, and the Ki value of 5 nM, which could cause a maximum of 100% inhibition [1].
Hydroxyprostaglandin dehydrogenase 15-(NAD), also called 15-hydroxy prostaglandin dehydrogenase (15-hydroxy PGDH), is a critical enzyme participated in the inactivation of prostaglandins (PGs) and related eiscosanoids. 15-hydroxy PGDH belongs to the family of oxidoreductases, specifically those acting on the CH-OH group of substrates with NAD+ or NADP+ as acceptor. 15-hydroxy PGDH could catalyze the oxidation of primary PGs to their 15-keto metabolites [2]. Radioimmunoassay for 15-hydroxy prostaglandin dehydrogenase had identified two types of enzyme activity, of which type-I used NAD+ as a cofactor, while type-II used NADP+ as a cofactor and bear wider substrate specificity [3].
In Vitro: no data available.
In Vivo: no data available.
Clinical trial: no data available.
References:
[1] Niesen F H, Schultz L, Jadhav A, et al. High-Affinity Inhibitors of Human NAD + -Dependent 15-Hydroxyprostaglandin Dehydrogenase: Mechanisms of Inhibition and Structure-Activity Relationships[J]. PLOS ONE, 2010, 5(11).
[2] Tai H, Ensor C M, Tong M, et al. Prostaglandin catabolizing enzymes.[J]. Prostaglandins & Other Lipid Mediators, 2002: 483-493.
[3] Lee S C, Levine L. Prostaglandin metabolism. II. Identification of two 15-hydroxyprostaglandin dehydrogenase types.[J]. Journal of Biological Chemistry, 1975, 250(2): 548-552.
| Cas No. | 355827-05-3 | SDF | |
| 化学名 | 2-[[(6-bromo-3H-imidazo[4,5-b]pyridin-2-yl)thio]methyl]-benzonitrile | ||
| Canonical SMILES | BrC1=CNC2=NC(SCC3=CC=CC=C3C#N)=NC2=C1 | ||
| 分子式 | C14H9BrN4S | 分子量 | 345.2 |
| 溶解度 | ≤12mg/ml in DMSO;14mg/ml in dimethyl formamide | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8969 mL | 14.4844 mL | 28.9687 mL |
| 5 mM | 0.5794 mL | 2.8969 mL | 5.7937 mL |
| 10 mM | 0.2897 mL | 1.4484 mL | 2.8969 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。
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