keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α/β的高效选择性抑制剂,IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性,对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外,CHIR-99021 HCl 是Wnt/β-catenin信号通路的强大激活剂。此外,它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外,拉杜维格西单盐酸盐诱导自噬[1][2][3]。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 343 | 现货 | ||
2 mg | ¥ 495 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,530 | 现货 | ||
50 mg | ¥ 2,320 | 现货 | ||
100 mg | ¥ 3,490 | 现货 | ||
200 mg | ¥ 4,970 | 现货 | ||
500 mg | ¥ 7,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | 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]. |
体外活性 | Laduviglusib monohydrochloride inhibits human GSK-3β with K i values of 9.8 nM [1]. Laduviglusib monohydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites. In vitro kinase assays expose that Laduviglusib monohydrochloride specifically inhibits GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM), with little effect on other kinases [4]. In the presence of Laduviglusib monohydrochloride the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib monohydrochloride with an IC 50 of 4.9 μM [2]. |
体内活性 | In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) monohydrochloride rapidly reduces plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration [1]. Laduviglusib (2 mg/kg) monohydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib monohydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX + cells, and improves crypt regeneration and villus height. Laduviglusib monohydrochloride treatment increases Lgr5 + cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h [5]. |
别名 | CT99021 HCl, Laduviglusib HCl |
分子量 | 501.8 |
分子式 | C22H19Cl3N8 |
CAS No. | 1797989-42-4 |
keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 54.0 mg/mL (107.6 mM), Sonication is recommended.
H2O: 6.4 mg/mL (12.8 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 1.9928 mL | 9.9641 mL | 19.9283 mL | 49.8206 mL |
5 mM | 0.3986 mL | 1.9928 mL | 3.9857 mL | 9.9641 mL | |
10 mM | 0.1993 mL | 0.9964 mL | 1.9928 mL | 4.9821 mL | |
DMSO | 20 mM | 0.0996 mL | 0.4982 mL | 0.9964 mL | 2.491 mL |
50 mM | 0.0399 mL | 0.1993 mL | 0.3986 mL | 0.9964 mL | |
100 mM | 0.0199 mL | 0.0996 mL | 0.1993 mL | 0.4982 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CHIR-99021 HCl 1797989-42-4 PI3K/Akt/mTOR signaling Stem Cells GSK-3 CT99021 HCl Laduviglusib HCl Inhibitor inhibitor inhibit