GSK481
目录号 : GC15573
A selective inhibitor of RIP1
Cas No.:1622849-58-4
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
IC50: 1.3 nM for RIP1
GSK481 is a receptor interacting protein kinase 1 (RIP1) inhibitor.
The role of RIP1 kinase in tumor necrosis factor mediated inflammation has resulted in its emergence as a promising target for the treatment of multiple inflammatory diseases.
In vitro: Previous study showed that GSK481 could not only trigger an increase in biochemical activity but also exhibit great translation in the U937 cellular assay with IC50 of 10 nM. Moreover, GSK481 also showed complete specificity for RIP1 kinase against all other tested kinases when profiled over both a P33 radiolabeled assay screen. In tight-binding ADP-Glo IC50 evaluation with increasing ATP concentration, GSK481 exhibited a shift to lower potency, which was corresponding to a competitive model. In addition, GSK481 was also found to be a potent inhibitor of S166 phosphorylation in wild-type human RIP1 but was ineffective at reducing S166 phosphorylation for wild-type mouse RIP1. GSK481 was also able to more potently inhibit Ser166 phosphorylation in all three tested mouse RIP1 mutants than in wild-type mouse [1].
In vivo: So far, there is no animal in vivo data reported for GSK481.
Clinical trial: Up to now, GSK481 is still in the preclinical development stage.
Reference:
[1] Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78.
| Cas No. | 1622849-58-4 | SDF | |
| 化学名 | (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide | ||
| Canonical SMILES | O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O | ||
| 分子式 | C21H19N3O4 | 分子量 | 377.39 |
| 溶解度 | DMF: 25 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2) (1:10): 0.09 mg/mL | 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 | 2.6498 mL | 13.2489 mL | 26.4978 mL |
| 5 mM | 0.53 mL | 2.6498 mL | 5.2996 mL |
| 10 mM | 0.265 mL | 1.3249 mL | 2.6498 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。