CHIR-99021 HCl NEW
| Price | $30 | $44 | $70 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: CHIR-99021 HCl | CAS No.: 1797989-42-4 |
| Purity: 98.44% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | CHIR-99021 HCl |
| 描述 | CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3]. |
| 體外活性 | Laduviglusib monohydrochloride is a potent inhibitor of human GSK-3β, demonstrating a K_i value of 9.8 nM. As a small organic molecule, it competitively inhibits GSK3α and GSK3β by binding to their ATP-binding sites. Kinase assay results reveal that Laduviglusib monohydrochloride specifically targets GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM) with minimal impact on other kinases. Studies show that at concentrations of 2.5 μM to 10 μM, Laduviglusib monohydrochloride significantly reduces the viability of ES-D3 cells in a dose-dependent manner, with an IC 50 of 4.9 μM, indicating a substantial reduction in cell viability at these concentrations. |
| 體內(nèi)活性 | In ZDF rats, administering a single oral dose of Laduviglusib monohydrochloride, either 16 mg/kg or 48 mg/kg, swiftly lowers plasma glucose levels, achieving a peak reduction of approximately 150 mg/dl within 3-4 hours post-dose [1]. Additionally, a one-time administration of Laduviglusib (2 mg/kg) monohydrochloride, 4 hours prior to exposure, markedly enhances survival rates following 14.5 Gy abdominal irradiation (ABI). This treatment significantly inhibits crypt cell apoptosis and the buildup of p-H2AX + cells, while fostering crypt regeneration and increasing villus height. Furthermore, Laduviglusib monohydrochloride enhances the survival of Lgr5 + cells by preventing apoptosis and effectively halts the early reduction of Olfm4, Lgr5, and CD44 markers, observable as soon as 4 hours post-treatment [5]. |
| 存儲(chǔ)條件 | keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 35 mg/mL (69.75 mM), Sonication is recommended. H2O : 6.4 mg/mL (12.8 mM), Sonication is recommended. |
| 關(guān)鍵字 | CHIR-99021 HCl |
| 相關(guān)產(chǎn)品 | PHA-767491 | Cromolyn sodium | GSK 3 Inhibitor IX | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | SNS-032 | GSK-3 Inhibitor 5 | MeBIO | 1-Azakenpaullone |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 神經(jīng)保護(hù)化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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