IWR-1-endo
(Synonyms: endo-IWR 1; IWR-1-endo) 目录号 : GC10950
IWR-1-endo 是一种有效的 Wnt 反应抑制剂，可阻断基于细胞的 Wnt/β-catenin 通路报告基因反应，IC50 值为 180 nM。
Cas No.:1127442-82-3
Sample solution is provided at 25 µL, 10mM.
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IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. IWR-1-endo induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing the Axin scaffold destruction complex[1].
IWR-1-endo (10 µM; 1h) attenuated the protective effect of Intermedin/adrenomedullin-2, inhibited cell motility and the number of migrating cells [2]; IWR-1-endo (0.2 µM; 6 days) reduced the protein expression of ALB, AFP, CYP3A4, β-catenin and TCF1 in the nucleus [3]. IWR-1-endo (5-50μM; 24h; 48h) reduced the proliferation of HCT116 cells in a dose- and time-dependent manner [4].
IWR-1-endo (10 μM, ip, q2d; 30 days) partially rescued the cardiomyocyte proliferation defect caused by impaired endocardial Notch signaling[5]. In vivo, IWR-1-endo (5 μM; 24 h) inhibited zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM. The IWR-1-exo diastereoisomer has much lower activity on the Wnt/β-catenin pathway and has been used as a control[6].
[1]. Lu J, Ma Z, Hsieh JC, Fan CW, Chen B, Longgood JC, Williams NS, Amatruda JF, Lum L, Chen C. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. [2]. [2].Wang Y, Wu Z, Tian J, Mi Y, Ren X, Kang J, Zhang W, Zhou X, Wang G, Li R. Intermedin protects HUVECs from ischemia reperfusion injury via Wnt/β-catenin signaling pathway. Ren Fail. 2019 Nov;41(1):159-166.
[3]. Gao W, Zhou P, Ma X, Tschudy-Seney B, Chen J, Magner NL, Revzin A, Nolta JA, Zern MA, Duan Y. Ethanol negatively regulates hepatic differentiation of hESC by inhibition of the MAPK/ERK signaling pathway in vitro. PLoS One. 2014 Nov 13;9(11):e112698.
[4]. Lee SC, Kim OH, Lee SK, Kim SJ. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. Oncotarget. 2015 Sep 29;6(29):27146-59.
[5]. Zhao L, Ben-Yair R, Burns CE, Burns CG. Endocardial Notch Signaling Promotes Cardiomyocyte Proliferation in the Regenerating Zebrafish Heart through Wnt Pathway Antagonism. Cell Rep. 2019 Jan 15;26(3):546-554.e5.
[6]. Lu J, Ma Z, Hsieh JC, Fan CW, Chen B, Longgood JC, Williams NS, Amatruda JF, Lum L, Chen C. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7.
IWR-1-endo 是一种有效的 Wnt 反应抑制剂，可阻断基于细胞的 Wnt/β-catenin 通路报告基因反应，IC50 值为 180 nM。IWR-1-endo通过稳定 Axin 支架破坏复合物诱导 Axin2 蛋白水平并促进 β-catenin 磷酸化[1]。
IWR-1-endo(10 µM；1h)减弱了Intermedin/adrenomedullin-2的保护作用，抑制了细胞运动能力和迁移细胞的数量[2]；IWR-1-endo(0.2 µM；6天)降低了细胞核内ALB、AFP、CYP3A4、β-catenin和TCF1的蛋白表达[3]。IWR-1-endo(5-50μM；24h；48h)以剂量和时间依赖性方式降低HCT116细胞的增殖[4]。
IWR-1-endo( 10μM , ip, q2d ; 30days )部分挽救了由心内膜Notch信号受损引起的心肌细胞增殖缺陷[5]。在体内试验中，IWR-1-endo （5 μM ; 24h）抑制斑马鱼尾鳍再生，最小抑制浓度为 0.5 μM。IWR-1-exo 非对映异构体对 Wnt/β-catenin 通路的活性要低得多，已被用作对照[6]。
| Cell experiment [1]: | |
Cell lines | HUVEC cell lines |
Preparation Method | The experiment was divided into groups as follow: untreated HUVECs in serum-free culture medium (normal); H/R model (H/R); HUVECs preincubated with IMD for 1 h at 37 °C then changed to culture medium as for the H/R group (H/R + IMD); HUVECs preincubated with IWR-1-endo in incubator for 1 h, then changed to culture medium as for the IMD + H/R group with IWR-1-endo added (H/R + IMD + IWR). |
Reaction Conditions | IWR-1-endo( 10 µM) ;1h |
Applications | IWR-1-endo attenuated the protective effect of Intermedin/adrenomedullin-2 and suppressed cell motility and the number of migrating cells. |
| Animal experiment [2]: | |
Animal models | Entricular apex resection modle |
Preparation Method | These animals were injected intraperitoneally with 25 μL of IWR-1-endo (10 μM in PBS) or DMSO (0.1% in PBS). The injection was performed at 5 dpa and 6 dpa for CM proliferation analysis at 7 dpa. For 30 dpa regeneration analysis, drugs were injected once every two days from 2 dpa throughout 30 dpa. |
Dosage form | IWR-1-endo ( 10μM , ip, q2d ) ; 30days |
Applications | IWR-1-endo partially rescues cardiomyocyte proliferation defects caused by impaired endocardial Notch signaling |
References: | |
| 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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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