STK16-IN-1
目录号 : GC32984
An inhibitor of STK16
Cas No.:1223001-53-3
Sample solution is provided at 25 µL, 10mM.
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STK16-IN-1 is an inhibitor of the serine/threonine kinase STK16 (IC50 = 295 nM).1 It is selective for STK16 over mTOR, PI3Kδ, and PI3Kγ in an enzyme assay (IC50s = 5,560, 856, and 867 nM, respectively) and over 440 additional kinases in a KinomeScan profiling assay. It decreases the growth of MCF-7 cells (GI50 = ~10 ?M) and increases the number of binucleated cells. STK16-IN-1 (2.5-5 ?M) potentiates the antiproliferative effects of colchicine , paclitaxel , doxorubicin , and cisplatin in MCF-7 cells.
1.Liu, F., Wang, J., Yang, X., et al.Discovery of a highly selective STK16 kinase inhibitorACS Chem. Biol.11(6)1537-1543(2016)
Kinase experiment: | STK16-IN-1 is generally prepared with 1:3 serial dilutions for 4 concentrations (100 nM, 50 nM, 20 nM, and 10 nM); 6 concentrations are used (1 mM to 10 μM) for ATP competition experiments. The kinase reaction is performed with 1×kinase reaction buffer. Reactions in each well are started immediately by adding ATP and kept going for half an hour under 37°C. After the plate cooled for 5 minutes at room temperature, 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ADP within 40 minutes. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 1 hour to produce a luminescence signal[1]. |
Cell experiment: | MCF-7, HCT116, HeLa cells are treated with STK16-IN-1 (0, 5, 10 μM) for 72 hours and apoptotic cells are analyzed by flow cytometry using Annexin V/PI apoptosis detection kit[1]. |
References: [1]. Liu F, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43. | |
| Cas No. | 1223001-53-3 | SDF | |
| Canonical SMILES | FC1=CC=C(N2C(C(C=CC2=O)=CN3)=C4C3=NC=C4)C=C1C | ||
| 分子式 | C17H12FN3O | 分子量 | 293.3 |
| 溶解度 | DMSO : 15 mg/mL (51.14 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 | 3.4095 mL | 17.0474 mL | 34.0948 mL |
| 5 mM | 0.6819 mL | 3.4095 mL | 6.819 mL |
| 10 mM | 0.3409 mL | 1.7047 mL | 3.4095 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet