CHIR-99021 (CT99021)

For research use only. Not for use in humans.

目录号:S1263

CHIR-99021 (CT99021) Chemical Structure

Molecular Weight(MW): 465.34

CHIR-99021 (CT99021)是一种GSK-3αGSK-3β抑制剂, IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性,对GSK-3β的选择性是对CDKs选择性的350倍。

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客户使用Selleck生产的CHIR-99021 (CT99021)发表文献322篇:

产品安全说明书

GSK-3抑制剂选择性比较

生物活性

产品描述 CHIR-99021 (CT99021)是一种GSK-3αGSK-3β抑制剂, IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性,对GSK-3β的选择性是对CDKs选择性的350倍。
靶点
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
体外研究

CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SW982 cell NI\UNYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHq3[3ZKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> M3GxZXNCVkeHUh?=
human GCT cell NVvX[WFjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGL3SHBKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwOk44OiCwTT6= NGTm[|FUSU6JRWK=
human 769-P cell M2niNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXm2PXZqUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5PC57OTDuUU4> M{m4fnNCVkeHUh?=
human LOXIMVI cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1jHPWlvcGmkaYTpc44hd2ZiaIXtZY4hVE:[SV3WTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5QC5|MjDuUU4> NFm1N3FUSU6JRWK=
human D-336MG cell MojhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnfDTY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFQ3NjJibl2u Ml;DV2FPT0WU
human S-117 cell NGjrU|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV;lboZTUW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> NYXNdHZwW0GQR1XS
human D-247MG cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjCTY5pcWKrdHnvckBw\iCqdX3hckBFNTJ2N13HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQ5NjV{IH7NMi=> NE\Nbo5USU6JRWK=
human TYK-nu cell MnzxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFc6KM7:TT6= NU\LOplKW0GQR1XS
human A498 cell NEfJWFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVPNUWZnUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{KM7:TT6= MUjTRW5ITVJ?
human HepG2 cells NHTEblZHfW6ldHnvckBie3OjeR?= MmLmN{Bp MVHJcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmOxcoDvdoF1cW:wIH;mJHs{UF2pbIXjc5NmKGmwdH:g[4x6[2:pZX6gZYZ1\XJiMzDodpMh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbne= M4rvb|IzOjZzMEKz
human BCPAP cell NHO3eZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HVU2lvcGmkaYTpc44hd2ZiaIXtZY4hSkOSQWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY4KM7:TT6= MofJV2FPT0WU
human KYSE-180 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLFTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> NFnGRolUSU6JRWK=
human MIA-PaCa-2 cell M{Dxb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnjCTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55NjFOwG0v MXLTRW5ITVJ?
human HCC1395 cell NE[4PJRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF|OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc5KM7:TT6= MWXTRW5ITVJ?
human RS4-11 cell NGP3PZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37PTWlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u MmDjV2FPT0WU
human NCI-H2122 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFy1XI9KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMkig{txONg>? MlPtV2FPT0WU
human SNU-423 cell NHvFflJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2nPXGlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi53IN88UU4> MnPYV2FPT0WU
human SK-LMS-1 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43PCEQvF2u M3q2THNCVkeHUh?=
human RPMI-7951 cell MlroS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkO2TY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNzFOwG0v NEfpTJhUSU6JRWK=
human COLO-829 cell MojHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4LJTGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24Nlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjd4NUSg{txONg>? M3HkOHNCVkeHUh?=
human SCC-9 cell NWLuRW9VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M33CSmlvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlk2KM7:TT6= M1rENXNCVkeHUh?=
human A704 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH;oTodKdmirYnn0bY9vKG:oIHj1cYFvKEF5MESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlA5OTJizszNMi=> NU\JZ2pqW0GQR1XS
human HOP-62 cell M2rlUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXHJcohq[mm2aX;uJI9nKGi3bXHuJGhQWC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|YxPTRizszNMi=> NG\LeXpUSU6JRWK=
human HCC1569 cell MlnUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\vbZlKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G1Olkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjR6M{C1JO69VS5? MXLTRW5ITVJ?
human A172 cell NWnq[XRIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWXJcohq[mm2aX;uJI9nKGi3bXHuJGEyPzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lke1OFk5KM7:TT6= NFzLe5hUSU6JRWK=
human MOLT-16 cell MnrXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1XzTmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDh3NU[g{txONg>? MWTTRW5ITVJ?
human TE-15 cell M2fqWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmToTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVU{PDNizszNMi=> MnXSV2FPT0WU
human OE19 cell Mn\4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUmyTXFoUW6qaXLpeIlwdiCxZjDoeY1idiCRRUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PjR3MTFOwG0v NV3rbVM{W0GQR1XS
human MHH-ES-1 cell NWK5PIxnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;5cmxKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yNEW0OUDPxE1w MnTOV2FPT0WU
human NKM-1 cell NGHUVFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoHrTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVM6PzFizszNMi=> MmjEV2FPT0WU
human RCC10RGB cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXfyTIJoUW6qaXLpeIlwdiCxZjDoeY1idiCUQ1OxNHJISiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMkm0O|kh|ryP MkHZV2FPT0WU
human BxPC-3 cell M1W4SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmW1TY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlcxOzlzIN88UU4> MXrTRW5ITVJ?
human ALL-PO cell Ml36S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnjSTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{QDV6IN88UU4> M{jqU3NCVkeHUh?=
human SK-OV-3 cell NH;PXZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlztTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46QTN2IN88UU4> M{DKeXNCVkeHUh?=
human SW1710 cell NXHsdZF7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHLhcFRKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? MlXTV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; 

PubMed: 30709379     


NCI-H460 cells were co-cultured with HUVECs in a 3D culture system, and then treated with 1 μM CHIR-99021, 10 μM or 20 μM Cisplatin, or a combination of both, for 24 h. Cells were harvested and immunoblotted with anti-cleaved PARP, anti-CD31, anti-VE-cadherin, anti-α-SMA, anti-vimentin, and anti-β-actin antibodies. 

CTNNB1; 

PubMed: 23993102     


Treatment with the GSK3β inhibitor CHIR-99021 led to increased levels of β-catenin in RKO and HT29 (non-mutant) cells.

β-catenin; 

PubMed: 24165128     


HeLa cells were treated with 5 μm CHIR-99021 for the indicated times. The samples were analyzed by Western blot.

30709379 23993102 24165128
Growth inhibition assay
Cell viability; 

PubMed: 22039301     


HMC-1.2 cells were cultured in the absence or presence of GSK3β inhibitor (CHIR 99021, 3-30 µM) and viability cell count was assessed by trypan blue dye exclusion after 24 h, 48 h or 72 h. All data are presented as the mean ± SEM of three independent experiments conducted in triplicate. p < 0.05*, p < 0.001** p < 0.0001*** vs vehicle treated control cells.

22039301
Immunofluorescence
SOX10/EdU; 

PubMed: 28174705     


Incorporation of EdU (white arrowheads) into SOX10+ ENS (enteric nervous system) cells with and without CHIR-99021.

Oct3/4; 

PubMed: 24779365     


Fluorescence micrographs showing the protein expression of Brachyury/Oct3/4 after a three day differentiation of ES-D3 cells with BIO (0.5 μM), SB-216763 (5 μM), CHIR-99021 (5 μM), or CHIR-98014 (1 μM). Nuclei were counterstained with DAPI (blue). The merge is shown in yellow. Original magnification 400x. Scale bar = 50 μm.

28174705 24779365
体内研究 Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge[1].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: Insulin receptor–expressing CHO-IR cells; Primary rat hepatocytes
  • Concentrations: 0.01-10 μM
  • Incubation Time: 30 min
  • Method:

    CHO-IR cells expressing human insulin receptor are grown to 80% confluence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 ml of medium without fetal bovine serum. After 24 h, medium is replaced with 1 ml of serum-free medium containing GSK-3 inhibitor or control (final DMSO concentration <0.1%) for 30 min at 37°C. Cells are lysed and centrifuged 15 min at 4°C/14000g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mmol/l glucose-6-phosphate, using the filter paper assay of Thomas et al.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: Female db/db mice; Male ZDF rats
  • Formulation: HCl salts formulated
  • Dosages: 8-48 mg/kg
  • Administration: oral administration
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 10 mg/mL warmed (21.48 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+ddH2O
3.5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 465.34
化学式

C22H18Cl2N8

CAS号 252917-06-9
储存条件 粉状
溶于溶剂
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID