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CHIR-99021 HCl

CHIR-99021 HCl

产品编号 T2310L   CAS 1797989-42-4
别名: CT99021 HCl, Laduviglusib HCl

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]。

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CHIR-99021 HCl Chemical Structure
CHIR-99021 HCl, CAS 1797989-42-4
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
其他形式的 CHIR-99021 HCl:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: CHIR-99021 HCl (T2310L)
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纯度: 98.07%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 54.0 mg/mL (107.6 mM), Sonification is recommended.

H2O: 6.4 mg/mL (12.8 mM), Sonification is recommended.

溶液配制表

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

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TargetMol Library Books参考文献

1. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95. 2. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273. 3. Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7(4):e35892. 4. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. 5. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.
GSK-3β inhibitor 14 CHIR-98014 Bakkenolide A 5-Iodo-indirubin-3'-monoxime BIP-135 BIO-acetoxime ALSTERPAULLONE GSK-3β inhibitor 1

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 药物功能重定位化合物库 抑制剂库 抗癌药物库 抗癌临床化合物库 激酶抑制剂库 经典已知活性库 临床期小分子药物库 神经元分化化合物库 抗癌化合物库

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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。

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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。

Keywords

CHIR-99021 HCl 1797989-42-4 PI3K/Akt/mTOR signaling Stem Cells GSK-3 CT99021 HCl Laduviglusib HCl Inhibitor inhibitor inhibit

 

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