YB-0158
(Synonyms: Wnt pathway inhibitor 2) 目录号 : GC63303
YB-0158 被称为 Wnt 通路抑制剂 2。
Cas No.:1144043-83-3
Sample solution is provided at 25 µL, 10mM.
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 |
HT29 cells |
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Preparation Method |
Cells were treated with DMSO or YB-0158 for 48 hours. As a positive control, each cell line was treated with 1 µM of staurosporine for 6 h. |
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Reaction Conditions |
0.2, 0.5µM for 48 hours |
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Applications |
EdU incorporation confirmed that lower doses of YB-0158 were sufficient to significantly decrease proliferation in human CRC cells. When used at 0.5 µM, YB-0158 also significantly increased apoptosis in CRC cells as represented by activated Caspase-3/7 detection assays |
| Animal experiment [1]: | |
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Animal models |
C57BL/6 mice accepted subcutaneous injection of MC38 cells into the flanks |
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Preparation Method |
Seven days post-injection, daily doses of YB-0158 (100mg/kg), or control saline (HBSS vehicle) were intraperitoneally injected in tumor-bearing animals for 14 days. |
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Dosage form |
Intraperitoneal injection, 100mg/kg |
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Applications |
No significant differences in primary tumor size were observed upon either YB-0158 in vivo treatments versus saline controls, residual secondary tumors from YB-0158-treated group were significantly smaller versus matched saline controls. |
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References: [1]: Angelique N. Masibag, Christopher J. Bergin, Joshua R. Haebe, AÏcha Zouggar, Muhammad S. Shah, Tamara Sandouka, Amanda Mendes da Silva, FranÇois M. Desrochers, Aube Fournier-Morin, Yannick D. Benoit.Pharmacological targeting of Sam68 functions in colorectal cancer stem cells. iScience, Volume 24, Issue 12, 17 December 2021, Pages 103442 |
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YB-0158 is known as Wnt pathway inhibitor 2. YB-0158 is a peptidomimetic structure with high predicted affinity for Sam68 [1].
YB-0158 elicits a cancer-selective response impeding main cancer stem cell hallmarks [1].
YB-0158 displayed enhanced selective toxicity in colorectal cancer models vs. normal intestinal epithelium progenitor cells. YB-0158 exert negative impact on cancer cell growth by inducing apoptosis and reducing proliferation. YB-0158 eradicated CSCs activity in vivo by a syngeneic mouse-to-mouse serial transplantation assay [2].
References:
[1]. Angelique N. Masibag, Christopher J. Bergin, Joshua R. Haebe, A?cha Zouggar, Muhammad S. Shah, Tamara Sandouka, Amanda Mendes da Silva, Fran?ois M. Desrochers, Aube Fournier-Morin, Yannick D. Benoit.Pharmacological targeting of Sam68 functions in colorectal cancer stem cells. iScience, Volume 24, Issue 12, 17 December 2021, Pages 103442
[2]. Masibag, Angelique Noelline. Characterization of a New Peptidomimetic Compound Modulating Sam68 Functions in Human Colon Cancer Stem Cells. Diss. Université d'Ottawa/University of Ottawa, 2021.
YB-0158 被称为 Wnt 通路抑制剂 2。YB-0158 是一种拟肽结构，对 Sam68 [1] 具有高预测亲和力。
YB-0158 引发癌症选择性反应，阻碍主要的癌症干细胞标志[1]。
与正常肠上皮祖细胞相比，YB-0158 在结直肠癌模型中表现出增强的选择性毒性。 YB-0158 通过诱导细胞凋亡和减少增殖对癌细胞生长产生负面影响。 YB-0158 通过同源小鼠对小鼠连续移植试验在体内根除 CSCs 活性[2]。
| Cas No. | 1144043-83-3 | SDF | |
| 别名 | Wnt pathway inhibitor 2 | ||
| 分子式 | C32H32N7Na2O7P | 分子量 | 703.59 |
| 溶解度 | DMSO : 100 mg/mL (142.13 mM; Need ultrasonic)|Water : < 0.1 mg/mL (ultrasonic;adjust pH to 1 with 1M HCl) (insoluble) | 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 | 1.4213 mL | 7.1064 mL | 14.2128 mL |
| 5 mM | 0.2843 mL | 1.4213 mL | 2.8426 mL |
| 10 mM | 0.1421 mL | 0.7106 mL | 1.4213 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。
Pharmacological targeting of Sam68 functions in colorectal cancer stem cells
iScience 2021 Nov 14;24(12):103442.PMID:34877499DOI:PMC8633986
Cancer stem cells (CSCs) are documented to play a key role in tumorigenesis and therapy resistance. Despite significant progress in clinical oncology, CSC reservoirs remain elusive and difficult to eliminate. Reverse-turn peptidomimetics were characterized as disruptors of CBP/beta-Catenin interactions and represent a promising avenue to curb hyperactive canonical Wnt/beta-Catenin signaling in CSCs. Recent studies suggested Sam68 as a critical mediator of reverse-turn peptidomimetics response in CSC populations. Using computational and biochemical approaches we confirmed Sam68 as a primary target of reverse-turn peptidomimetics. Furthermore, we executed an in silico drug discovery pipeline to identify yet uncharacterized reverse-turn peptidomimetic structures displaying superior anti-CSC activity in transformed pluripotent and colorectal cancer cell models. Thus, we identified YB-0158 as a reverse-turn peptidomimetic small molecule with enhanced translational potential, altering key hallmarks of human colorectal CSCs in patient-derived ex vivo organoids and in vivo serial tumor transplantation.