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CHIR-99021

目录号 M1692 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂, IC50分别为10 nM and 6.7 nM。

CHIR-99021结构式

别名:CT99021

包装 价格 库存状态
2mg 原价 ¥ 737
促销价 ¥ 700.15
中国库存现货
5mg 原价 ¥ 1100
促销价 ¥ 1045
中国库存现货
10mg 原价 ¥ 1430
促销价 ¥ 1358.5
中国库存现货
50mg 原价 ¥ 3300
促销价 ¥ 3135
中国库存现货
100mg 原价 ¥ 6380
促销价 ¥ 6061
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂, IC50分别为10 nM and 6.7 nM。CHIR-99021作用于GSK-3比作用于其最接近的同系物CDC2和ERK2,及其他蛋白激酶选择性高500倍。此外,CHIR-99021只与一组22种药理相关的受体微弱结合,且对一组23种非激酶的酶几乎没有抑制活性。CHIR-99021作用于表达胰岛素受体的CHO-IR细胞,诱导糖原合成酶(GS)激活,EC50为0.763 μM。

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 J1 mESCs or F9 mEC cells
方法 Immunofluorescence staining The expression and subcellular localisation of β-catenin in J1 mESCs treated with 1 μM BIO or 3 μM CHIR for 24 h was detected by immunofluorescence staining. Nuclei were stained with DAPI. J1 mESCs or F9 mEC cells were fixed and permeabilized using immunostaining fixation buffer and then blocked in blocking buffer (Beyotime Institute of Biotechnology). Subsequently, cells were incubated with the indicated primary antibody overnight at 4°C, followed by three washes with washing buffer (Beyotime Institute of Biotechnology) for 5 min and then incubation with an Alexa Fluor 555-conjugated secondary antibody for 2 h at room temperature. Nuclei were stained with DAPI. Cells were photographed under an inverted fluorescence microscope (Nikon, Tokyo, Japan).
浓度 3µM
处理时间 24h
动物实验
动物模型 Akita type 1 diabetic mice and wild-type mice
配制 DMSO
剂量 50 mg/kg, daily
给药处理 Intraperitoneal injection
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 465.34
分子式 C22H18Cl2N8
CAS号 252917-06-9
纯度 >99%
溶解性(25°C) DMSO 16 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.149 mL 10.7448 mL 21.4897 mL
5 mM 0.4298 mL 2.149 mL 4.2979 mL
10 mM 0.2149 mL 1.0745 mL 2.149 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Sci Rep (2015). Figure 3. CHIR-99021
方法 qPCR
细胞系 J1 mESCs and F9 mEC cells
浓度 3 μM
处理时间 24 h
实验结果 By contrast, all of the ESCC miRNAs were downregulated by CHIR (Fig. 3a–e). The miR-200b-429 and miR-183-182 clusters, which are highly expressed in pluripotent cells, were downregulated by both BIO and CHIR (Fig. 3f, 3g).
数据来源 Sci Rep (2015). Figure 1. CHIR-99021
方法 immunofluorescence staining
细胞系 J1 mESCs and F9 mEC cells
浓度 3 μM
处理时间 24 h
实验结果 The relativemRNA expression level of Nanog was determined in response to BIO or CHIR in J1mESCs and F9mEC cells by qPCR. As expected, transcription of Nanog in J1 mESCs and F9 mEC cells was upregulated by both BIO and CHIR
参考文献

Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains.
Ye, et al. PLoS One. 2012;7(4):e35892. PMID: 22540008.

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关键词:CHIR-99021, CT99021, CHIR-99021供应商, GSK-3抑制剂, 购买CHIR-99021, CHIR-99021结构式

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