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Laduviglusib trihydrochloride

Laduviglusib trihydrochloride

产品编号 T22657   CAS 1782235-14-6
别名: CT99021 trihydrochloride, CHIR 99021 trihydrochloride, CHIR 99021 trihydrochloride (252917-06-9 free base)

Laduviglusib trihydrochloride (CT99021 trihydrochloride) 是一种选择性糖原合成酶激酶 3 (GSK-3) 抑制剂,对 GSK-3α 和 GSK-3β 的 IC50 分别为 10 nM 和 6.7 nM。 Laduviglusib trihydrochloride 抑制人 GSK-3β,Ki 为 9.8 nM。 Laduviglusib trihydrochloride 是 Wnt/β-catenin 信号通路的激活剂。 Laduviglusib trihydrochloride 诱导自噬

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Laduviglusib trihydrochloride Chemical Structure
Laduviglusib trihydrochloride, CAS 1782235-14-6
规格 价格/CNY 货期 数量
1 mg ¥ 372 现货
2 mg ¥ 538 现货
5 mg ¥ 781 现货
10 mg ¥ 1,280 现货
25 mg ¥ 2,390 现货
50 mg ¥ 3,690 现货
100 mg ¥ 5,320 现货
500 mg ¥ 10,800 现货
1 mL * 10 mM (in DMSO) ¥ 937 现货
其他形式的 Laduviglusib trihydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Laduviglusib trihydrochloride (T22657)
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纯度: 99.03%
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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 Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor with IC50s of 10 nM and 6.7 nM for GSK-3α and GSK-3β. Laduviglusib trihydrochloride inhibits human GSK-3β with a Ki of 9.8 nM. Laduviglusib trihydrochloride is an activator of Wnt/β-catenin signaling. Laduviglusib trihydrochloride induces autophagy.
靶点活性 GSK-3α:10 nM, GSK-3β:6.7 nM, CDC2:8800 nM
体外活性 Laduviglusib trihydrochloride(10 μM) lowers the viability of the ES-D3 cells by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% with an IC50 of 4.9 μM[2]. Laduviglusib trihydrochloride shows >500-fold selectivity over ERK2, CDC2, and other protein kinases. Laduviglusib trihydrochloride specifically inhibits GSK3β and GSK3α with IC50s of 5nM and 10nM in vitro kinase assays[4].
体内活性 Oral administration of Laduviglusib trihydrochloride(16 mg/kg and 48 mg/kg) rapidly reduces plasma glucose with a maximal reduction of nearly 150 mg/dl in ZDF rats[1]. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride (2 mg/kg) improves survival after 14.5 Gy abdominal irradiation. Laduviglusib trihydrochloride inhibits crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride blocks apoptosis, increases Lgr5+ cell survival and prevents the reduction of Olfm4, Lgr5 and CD44[5].
别名 CT99021 trihydrochloride, CHIR 99021 trihydrochloride, CHIR 99021 trihydrochloride (252917-06-9 free base)
分子量 574.72
分子式 C22H21Cl5N8
CAS No. 1782235-14-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 17.1 mg/mL (29.8 mM), Sonication and heating are recommended.

DMSO: 28.8 mg/mL (50.1 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.74 mL 8.6999 mL 17.3998 mL 43.4994 mL
5 mM 0.348 mL 1.74 mL 3.48 mL 8.6999 mL
10 mM 0.174 mL 0.87 mL 1.74 mL 4.3499 mL
20 mM 0.087 mL 0.435 mL 0.87 mL 2.175 mL
DMSO 50 mM 0.0348 mL 0.174 mL 0.348 mL 0.87 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.
KenPaullone PHA-767491 hydrochloride CHIR-99021 HCl LY2090314 KY19382 PF-04802367 GS87 A-443654

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 激酶抑制剂库 抗肥胖化合物库 代谢化合物库 抗癌化合物库 细胞骨架化合物库 已知活性化合物库 经典已知活性库

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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。

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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

Laduviglusib trihydrochloride 1782235-14-6 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Stem Cells GSK-3 Wnt/beta-catenin 252917-06-9 free base CHIR 99021 Trihydrochloride CT99021 trihydrochloride Laduviglusib CHIR99021 Trihydrochloride CT99021 Trihydrochloride CT-99021 Trihydrochloride CT 99021 Trihydrochloride CT99021 CHIR 99021 CHIR 99021 trihydrochloride CHIR 99021 trihydrochloride (252917-06-9 free base) 252917-06-9 CHIR99021 CHIR-99021 CHIR-99021 Trihydrochloride CT-99021 Laduviglusib Trihydrochloride CT 99021 Inhibitor inhibitor inhibit

 

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