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GSK-3 糖尿病
/ CHIR 99021

CHIR 99021 99%+

货号：A133052 同义名： CT99021;Laduviglusib Ambeed 开学季，买赠积分，赢豪礼

Laduviglusib (CHIR-99021)是一种有效、选择性且具有口服活性的 GSK-3α/β 抑制剂，可用作细胞疗法中的辅助试剂。

CHIR 99021 化学结构 CAS号：252917-06-9
CHIR 99021 化学结构
CAS号：252917-06-9
CHIR 99021 3D分子结构
CAS号：252917-06-9
CHIR 99021 化学结构 CAS号：252917-06-9
CHIR 99021 3D分子结构 CAS号：252917-06-9
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CHIR 99021 纯度/质量文件 产品仅供科研

货号：A133052 标准纯度： 99%+
批次查询： 批次纯度:

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产品名称 GSK-3 ↓ GSK-3α ↓ GSK-3β ↓ 其他靶点 纯度
AZD2858 +

GSK-3, IC50: 68 nM

 		98+%
Bikinin ✔ 99%+
GSK 3 Inhibitor IX ++++

GSK-3, IC50: 5 nM

 		99%+
AZD1080 +++

GSK-3α, IC50: 6.9 nM

 		++

GSK-3β, IC50: 31 nM

 		99%+
BIO-acetoxime +++

GSK-3α, IC50: 10 nM

 		+++

GSK-3β, IC50: 10 nM

 		95%
SB-216763 ++

GSK-3α, IC50: 34.3 nM

 		++

GSK-3β, IC50: ~34.3 nM

 		98%
SB 415286 +

GSK-3α, IC50: 78 nM

 		+

GSK-3β, IC50: ~78 nM

 		99%+
CHIR-98014 ++++

GSK-3α, IC50: 0.65 nM

 		++++

GSK-3β, IC50: 0.58 nM

 		98%
LY2090314 ++++

GSK-3α, IC50: 1.5 nM

 		++++

GSK-3β, IC50: 0.9 nM

 		99%+
CHIR 99021 +++

GSK-3α, IC50: 10 nM

 		++++

GSK-3β, IC50: 6.7 nM

 		99%+
TDZD-8 +

GSK-3β, IC50: 2 μM

 		99%+
Indirubin +

GSK-3β, IC50: 0.6 μM

 		98%
IM-12 ++

GSK-3β, IC50: 53 nM

 		98%
TWS119 ++

GSK-3β, IC50: 30 nM

 		98%
1-Azakenpaullone +++

GSK-3β, IC50: 18 nM

 		99%+
AR-A014418 ++

GSK-3β, Ki: 38 nM

 		99%+
Tideglusib +

GSK-3β, IC50: 60 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

CHIR 99021 生物活性

靶点

  • GSK-3α

    GSK-3α, IC50:10 nM

  • GSK-3β

    GSK-3β, IC50:6.7 nM
描述 GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase, consisting of GSK-3α andβsubunit, which plays a key role in many different biological processes including tumorigenesis, cell survival, and developmental patterning. GSK-3 is constitutively active in non-stimulated cells and can negatively regulate canonical Wnt/β-catenin signaling. CHIR 99021 （CT99021）is highly selective aminopyrimidine-derivatived inhibitor of GSK-3 with IC50 of 10nM and 6.7nM for GSK-3α and GSK-3β(measured by kinase assays), respectively, and exhibits >500-fold selectivity for GSK-3 over closely related kinases, such as cdc2[8]Bennett CN, Ross SE, Longo KA, Bajnok L, Hemati N, Johnson KW, Harrison SD, MacDougald OA. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. doi: 10.1074/jbc.M204527200. Epub 2002 Jun 7. PMID: 12055200. https://pubmed.ncbi.nlm.nih.gov/12055200/. CHIR-99021 can mimic Wnt signaling in preadipocytes. Analysis of cytosolic and membranous fractions show that the free cytosolic -catenin was evaluated in 3T3-L1 preadipocytes treated with 3uM CHIR-99021 for 4 h [4]. Chir-99021 can activate glycogen synthase in cells. The concentrations of CHIR-99021 causing half-maximal glycogen synthase stimulation (EC50) were 76 nmol/l for CHO-IR cells. A single oral dose of CHIR 99021 (30mg/kg) rapidly lowered plasma glucose in ZDF rats[8]. In combination with different small molecules, CHIR-99021 can facilitate cardiomyocyte differentiation from human embryonic stem cells and iPS cells[10][9], reprogramming, like generation of functional astrocytes from mammalian fibroblasts[10] and maintaining undifferentiated mouse ES cells in the absence of LIF[11].
作用机制 CHIR 99021 can inhibit GSK3 by competing for their ATP-binding sites.

CHIR 99021 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human 769-P cell Growth inhibition assay Inhibition of human 769-P cell growth in a cell viability assay, IC50=584.99 nM. SANGER
human A172 cell Growth inhibition assay Inhibition of human A172 cell growth in a cell viability assay, IC50=3.75498 μM. SANGER
human A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=1.3 μM. SANGER
human A704 cell Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50=3.0812 μM. SANGER

CHIR 99021 动物研究

Dose Rat[3] (p.o.): 16 mg/kg - 48 mg/kg
Administration p.o.
Pharmacokinetics
Animal Mice[7]
Cmax 15.09 μM
T1/2 0.87 h
AUC 10.93 μM/kg·h

CHIR 99021 参考文献

[1]Martinez A, Castro A, et al. Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation. Med Res Rev. 2002 Jul;22(4):373-84.

[2]Bennett CN, Ross SE, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. Epub 2002 Jun 7.

[3]Ring DB, Johnson KW, 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.

[4]Lian X, Zhang J, et al. Directed cardiomyocyte differentiation from human pluripotent stem cells by modulating Wnt/β-catenin signaling under fully defined conditions. Nat Protoc. 2013 Jan;8(1):162-75.

[5]Tian E, Sun G, et al. Small-Molecule-Based Lineage Reprogramming Creates Functional Astrocytes. Cell Rep. 2016 Jul 19;16(3):781-92.

[6]Ying QL, Wray J, et al. The ground state of embryonic stem cell self-renewal. Nature. 2008 May 22;453(7194):519-23.

[7]CHIR99021 attenuates mood-related behaviors in lithium responsive and non responsive

[8]Ring DB, Johnson KW, Henriksen EJ, Nuss JM, Goff D, Kinnick TR, Ma ST, Reeder JW, Samuels I, Slabiak T, Wagman AS, Hammond ME, Harrison SD. 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. doi: 10.2337/diabetes.52.3.588. PMID: 12606497.

[9]Lian X, Zhang J, Azarin SM, Zhu K, Hazeltine LB, Bao X, Hsiao C, Kamp TJ, Palecek SP. Directed cardiomyocyte differentiation from human pluripotent stem cells by modulating Wnt/β-catenin signaling under fully defined conditions. Nat Protoc. 2013 Jan;8(1):162-75. doi: 10.1038/nprot.2012.150. Epub 2012 Dec 20. PMID: 23257984; PMCID: PMC3612968.

[10]Lian X, Hsiao C, Wilson G, Zhu K, Hazeltine LB, Azarin SM, Raval KK, Zhang J, Kamp TJ, Palecek SP. Robust cardiomyocyte differentiation from human pluripotent stem cells via temporal modulation of canonical Wnt signaling. Proc Natl Acad Sci U S A. 2012 Jul 3;109(27):E1848-57. doi: 10.1073/pnas.1200250109. Epub 2012 May 29. PMID: 22645348; PMCID: PMC3390875.

[11]Ying QL, Wray J, Nichols J, Batlle-Morera L, Doble B, Woodgett J, Cohen P, Smith A. The ground state of embryonic stem cell self-renewal. Nature. 2008 May 22;453(7194):519-23. doi: 10.1038/nature06968. PMID: 18497825; PMCID: PMC5328678.

CHIR 99021 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.49mL

4.30mL

2.15mL

CHIR 99021 技术信息

CAS号252917-06-9
分子式C22H18Cl2N8
分子量 465.338
别名 CT99021;Laduviglusib
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 16 mg/mL(34.38 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 55 mg/mL suspension

Tags: Laduviglusib | 252917-06-9 | CHIR-99021 | CT99021 | CHIR99021 | CHIR 99021 | CT99021 | CT 99021 | CT-99021 | GSK-3α/β Inhibitor (GMP) | PI3K/Akt/mTOR | Stem Cell/Wnt | Autophagy | GSK-3 | Wnt | β-catenin | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | CHIR 99021 纯度/质量文件 | CHIR 99021 亚型比较 | CHIR 99021 生物活性 | CHIR 99021 细胞研究 | CHIR 99021 动物研究 | CHIR 99021 参考文献 | CHIR 99021 实验方案 | CHIR 99021 技术信息

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