IWP-2-V2
(Synonyms: Inhibitor of Wnt Production-2-V2) 目录号 : GC14546
An inhibitor of Wnt production
Cas No.:877618-79-6
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: 27 nM
IWP-2-V2 is a Wnt production inhibitor.
Wnt signaling proteins are small secreted proteins that are active in tissue homeostasis, embryonic development, and tumorigenesis. Wnt proteins bind to receptors, initiating a signaling cascade that results in β-catenin activation of gene transcription.
In vitro: IWP-2 was identified as an inhibitor of Wnt production inactivating porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity was essential for the signaling ability and secretion of Wnt proteins. IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound. IWP-2-V2 was used to evaluate which structural features of IWP-2 were critical for impairing Wnt/β-catenin pathway activity [1].
In vivo: In CCI rats, repetitive i.t. administration of IWP-2 (20 μM) in the early phase could significantly delay production of mechanical allodynia. The same drug administrated in the late phase produced long-lasting inhibitory effects on the established mechanical allodynia. Such analgesia lasted 4–6 days for IWP-2 after termination of the third treatment. These results showed similar inhibitory effects of IWP-2 on thermal hyperalgesia after CCI treatment [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] B. Chen, M. E. Dodge, W. Tang, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature Chemical Biology 5(2), 100-107 (2009).
[2] Y. Zhang et al. WNT signaling underlies the pathogenesis of neuropathic pain in rodents. J Clin Invest. 2013 May 1; 123(5): 2268–2286.
| Cas No. | 877618-79-6 | SDF | |
| 别名 | Inhibitor of Wnt Production-2-V2 | ||
| 化学名 | N-(6-methyl-2-benzothiazolyl)-2-[[3,4,6,7-tetrahydro-4-oxo-3-(phenylmethyl)thieno[3,2-d]pyrimidin-2-yl]thio]-acetamide | ||
| Canonical SMILES | O=C(CSC(N1CC2=CC=CC=C2)=NC3=C(SCC3)C1=O)NC4=NC5=C(C=C(C)C=C5)S4 | ||
| 分子式 | C23H20N4O2S | 分子量 | 480.6 |
| 溶解度 | ≤2mg/ml in DMSO;5mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0807 mL | 10.4037 mL | 20.8073 mL |
| 5 mM | 0.4161 mL | 2.0807 mL | 4.1615 mL |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0807 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。