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CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。
别名：CT99021
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。
| 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 |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 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。
| 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 |
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 |
Stem Cells. 2019 Apr;37(4):516-528.
Human Multipotent Stromal Cell Secreted Effectors Accelerate Islet Regeneration.
CHIR-99021购买自AbMole
 |
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 |
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.
| 其他相关的GSK-3产品 |
|---|
| Bikinin
Bikinin is a strong activator of brassinosteroid (BR) signaling. |
| BIO
6-bromoindirubin-3′-oxime (BIO) is a potent, reversible and ATP-competitive GSK-3α/β inhibitor and the first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells. |
| CHIR 99021 trihydrochloride
CHIR 99021 trihydrochloride is a hydrochloride salt of CHIR 99021; selective GSK-3 inhibitor. |
| IM-12
IM-12是一种选择性的GSK-3β有效抑制剂，其IC50为53 nM。相比SB-216763，活性相当甚至要更好。 |
| SB415286
SB415286是一种有效的GSK3α抑制剂，IC50/Ki为78 nM/31 nM，也等效抑制GSK-3β。 |
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