QS 11
目录号 : GC17251
An ARFGAP inhibitor
Cas No.:944328-88-5
Sample solution is provided at 25 µL, 10mM.
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EC50: 1.5 μM for ARFGAP1 enzymatic assay [1] and 0.5 μM for Wnt synergist [2]
Purine derivative QS11 is a Wnt synergistic agonist by inhibiting the GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1). ARFGAP1 promotes hydrolysis of ARF1-bound GTP and is required in membrane trafficking and /or vesicle transport.
In vitro: QS11 showed potent Wnt Synergist activity with little cytotoxicity in HEK293 cells (EC50 = 0.5 μM) and human primary fibroblast cells (EC50 ≥ 10 μM). QS11 at 2.5 μM activated the Super(8X)TOPFlash reporter ~200-fold in the presence of Wnt-3a conditioned medium. Synergistic effect was also observed when QS11 was combined with recombinant Wnt-3a protein (10–200 ng/ml) [2].
In vivo: In Wnt signaling test model, embryos were injected with QS11, XWnt-8 RNA or a combination of QS11and XWnt-8 RNA. Compared with QS11 alone and XWnt-8 RNA alone, injection of a combination of XWnt-8 RNA and QS11 induced significantly more full (20.9%) and partial (30.2%) double axis formation [2]..
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Singh MK1, Gao H1, Sun W1, Song Z1, Schmalzigaug R2, Premont RT2, Zhang Q3. Structure-activity relationship studies of QS11, a small molecule Wnt synergistic agonist. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4838-42.
[2] Zhang Q1, Major MB, Takanashi S, Camp ND, Nishiya N, Peters EC, Ginsberg MH, Jian X, Randazzo PA, Schultz PG, Moon RT, Ding S. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7444-8. Epub 2007 Apr 25.
Cell experiment: | ARF-GTP levels are measured by using the GGA binding assay. NIH 3T3 cells are treated with QS11 or QS11-NC at the indicated concentrations for 36 h. Cells are lysed in ARF assay lysis buffer [50 mM Tris·HCl (pH 7.5), 100 mM NaCl, 2 mM MgCl2, 0.1% SDS, 0.5% sodium deoxycholate, 1% Triton X-100, 10% glycerol, and protease inhibitors]. GTP-bound ARF is assayed by its binding to a GST fusion protein, which contains the VHS domain to the GAT region of an ARF effector GGA3[1]. |
References: [1]. Zhang Q, et al. Small-molecule synergist of the Wnt/beta-catenin signaling pathway. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7444-8. | |
| Cas No. | 944328-88-5 | SDF | |
| 化学名 | (S)-2-((9-([1,1'-biphenyl]-4-ylmethyl)-2-((2,3-dihydro-1H-inden-5-yl)oxy)-9H-purin-6-yl)amino)-3-phenylpropan-1-ol | ||
| Canonical SMILES | OC[C@H](CC1=CC=CC=C1)NC2=NC(OC3=CC=C4CCCC4=C3)=NC5=C2N=CN5CC6=CC=C(C7=CC=CC=C7)C=C6 | ||
| 分子式 | C36H33N5O2 | 分子量 | 567.68 |
| 溶解度 | DMSO: <100 mM,Ethanol: <100 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 | 1.7616 mL | 8.8078 mL | 17.6156 mL |
| 5 mM | 0.3523 mL | 1.7616 mL | 3.5231 mL |
| 10 mM | 0.1762 mL | 0.8808 mL | 1.7616 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet