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YB-0158 Sale

(Synonyms: Wnt pathway inhibitor 2) 目录号 : GC63303

YB-0158 被称为 Wnt 通路抑制剂 2。

YB-0158 Chemical Structure

Cas No.:1144043-83-3

规格 价格 库存 购买数量
5 mg
¥6,380.00
现货
10 mg
¥10,200.00
现货
50 mg
¥35,620.00
现货
100 mg
¥57,000.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

HT29 cells

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.

Reaction Conditions

0.2, 0.5µM for 48 hours

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 [2]:

Animal models

C57BL/6 mice accepted subcutaneous injection of MC38 cells into the flanks

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.

Dosage form

Intraperitoneal injection, 100mg/kg

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.

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

产品描述

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]

Chemical Properties

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
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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。
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溶解性数据

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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
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Research Update

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.