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Laduviglusib,IC-0121293
Click£º1872     Release date£º2020-6-25    Author£ºAdministrator    Source£ºOriginal

Laduviglusib,IC-0121293



Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3¦Á/¦Â inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/¦Â-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy[1][2][3].
Cell Viability Assay[2]

Cell Line: ES-D3 cells
Concentration: 1-10 ¦̀M
Incubation Time: 3 days
Result: Reduced the viability of the ES-D3 cells by 24.7% at 2.5 ¦̀M, 56.3% at 5 ¦̀M, 61.9% at 7.5 ¦̀M and 69.2% at 10 ¦̀M
Animal Model: ZDF rats[1]
Dosage: 30 mg/kg
Administration: Oral administration
Result: Lowered plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration.
Animal Model: WT C57BL/6 mice[5]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Blocked crypt apoptosis and increased Lgr5+ cell survival.
[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate 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.

Order Information

Cat./REF.

Size

Price($£©

Price(€)

Price(£¤/CNY£©

Price(£¤/JYP£©

IC-0121293

5mg

$120.00

€ 144.00

£¤1,200.00

£¤23,880.00

IC-0121293

25mg

$480.00

€ 576.00

£¤4,800.00

£¤95,520.00

IC-0121293

100mg

$1,440.00

€ 1,728.00

£¤14,400.00

£¤286,560.00

 


On an article£ºNRF2 Inhibitor,IC-0199622
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