IWR-1-endo
(Synonyms: endo-IWR 1; IWR-1-endo) 目录号 : GC10950
Inhibitor of Wnt response
Cas No.:1127442-82-3
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
| Cell experiment [1]: | |
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Cell lines |
DLD-1 colorectal cancer (CRC) cell line |
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Preparation method |
The solubility of this compound in DMSO is >20.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1 μM, 2.5 μM, 10 μM |
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Applications |
IWR-1-endo promoted β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo blocked aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss. |
| Animal experiment [1]: | |
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Animal models |
Zebrafish |
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Dosage form |
10 mM, 24 h |
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Application |
IWR-1-endo inhibited tailfin regeneration and epithelial stem cell self-renewal in zebrafish. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. |
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IWR-1-endo is a small molecule inhibitor of Wnt Response with IC50 value of 180nM [1].
IWR-1-endo is a small molecule antagonists of the Wnt/β-catenin pathway screened out from a diverse synthetic chemical library. It acts as an inhibitor of Wnt response. IWR-1-endo can inhibit the activity of Wnt1, 2 and 3. In cultured cells, IWR-1-endo inhibits Wnt-induced β-catenin accumulation which is a downstream event of Lrp6 and Dvl2. It is proved that IWR-1-endo promote β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo is also shown to inhibit tailfin regeneration and epithelial stem cell self-renewal in zebrafish. These two processes are both dependent on Wnt/β-catenin signaling. Furthermore, IWR-1-endo can block aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss [1].
IWR-1-endo是一种Wnt反应的小分子抑制剂，其IC50值为180nM [1]。
IWR-1-endo是从多种合成化学库中筛选出的Wnt/β-catenin途径的小分子拮抗剂。它作为Wnt反应的抑制剂。IWR-1-endo可以抑制Wnt1、2和3的活性。在培养的细胞中，IWR-1-endo抑制了Wnt诱导的β-catenin积累，这是Lrp6和Dvl2的下游事件。证明了IWR-1-endo通过促进DLD-1结直肠癌细胞株中的Axin支架的破坏复合物的稳定性促进β-catenin的破坏。 IWR-1-endo还显示可以抑制斑马鱼的尾鳍再生和上皮干细胞自我更新。这两个过程都依赖于Wnt/β-catenin信号。此外，IWR-1-endo可以阻止由于Apc丧失而导致的Wnt/β-catenin的高度活化支持的异常细胞生长 [1]。
References:
[1] Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.
| Cas No. | 1127442-82-3 | SDF | |
| 别名 | endo-IWR 1; IWR-1-endo | ||
| 化学名 | 4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)-N-(quinolin-8-yl)benzamide | ||
| Canonical SMILES | O=C([C@@]1([H])[C@]2([H])[C@]3([H])C([H])([H])[C@@]1([H])C([H])=C3[H])N(C4=C([H])C([H])=C(C(N([H])C5=C([H])C([H])=C([H])C6=C5N=C([H])C([H])=C6[H])=O)C([H])=C4[H])C2=O | ||
| 分子式 | C25H19N3O3 | 分子量 | 409.44 |
| 溶解度 | ≥ 20.45mg/mL in DMSO | 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 | 2.4424 mL | 12.2118 mL | 24.4236 mL |
| 5 mM | 0.4885 mL | 2.4424 mL | 4.8847 mL |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4424 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。