HS-1371
目录号 : GC32280
A RIPK3 inhibitor
Cas No.:2158197-70-5
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
HS-1371 is a receptor-interacting serine/threonine kinase 3 (RIPK3) inhibitor (IC50 = 20.8 nM).1 It inhibits basal RIPK3 autophosphorylation and TNF-α- or TRAIL-induced necroptosis in HT-29 cells when used at a concentration of 5 ?M. It also inhibits necroptosis induced by a TNF-α Smac mimetic and the caspase inhibitor Z-VAD in HeLa cervical and NCI-H2009 lung cancer cells ectopically expressing RIPK3.
1.Park, H.-H., Park, S.-Y., Mah, S., et al.HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosisExp. Mol. Med.50(9)1-15(2018)
| Cas No. | 2158197-70-5 | SDF | |
| Canonical SMILES | CC1=CC=C(OC2=CC=NC3=CC(C4=CN(C5CCNCC5)N=C4)=CC=C23)C=C1 | ||
| 分子式 | C24H24N4O | 分子量 | 384.47 |
| 溶解度 | DMSO : 16.67 mg/mL (43.36 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 | 2.601 mL | 13.0049 mL | 26.0098 mL |
| 5 mM | 0.5202 mL | 2.601 mL | 5.202 mL |
| 10 mM | 0.2601 mL | 1.3005 mL | 2.601 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。
HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis
Exp Mol Med 2018 Sep 20;50(9):1-15.PMID:30237400DOI:PMC6148246
Necroptosis is a type of programmed cell death that usually occurs under apoptosis-deficient conditions. Receptor-interacting protein kinase-3 (RIP3, or RIPK3) is a central player in necroptosis, and its kinase activity is essential for downstream necroptotic signaling events. Since RIP3 kinase activity has been associated with various diseases, the development of specific RIP3 inhibitors is an attractive strategy for therapeutic application. In this study, we identified a potent RIP3 inhibitor, HS-1371, by the extensive screening of chemical libraries focused on kinases. HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner, providing a mechanism of action. Moreover, the compound inhibited TNF-induced necroptosis but did not inhibit TNF-induced apoptosis, indicating that this novel inhibitor has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity. Our results suggest that HS-1371 could serve as a potential preventive or therapeutic agent for diseases involving RIP3 hyperactivation.