CHIR-99021 (CT99021)

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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客户使用该产品的2个实验数据:

  • Lu1205 were treated with protein kinase inhibitors. Cell cycle protein expression was analyzed by western blot.

    Med Oncol, 2017, 35(1):7. CHIR-99021 (CT99021) purchased from Selleck.

    For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells. 

    Dr. Yong-Weon Yi from Georgetown University Medical Center. CHIR-99021 (CT99021) purchased from Selleck.

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 MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mk\5TY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxOE4yPiCwTT6= MoLCV2FPT0WU
human GCT cell NX;zeJJuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHPZWIVKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwOk44OiCwTT6= NXfZeHU6W0GQR1XS
human 769-P cell NUfHSmJHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYKyd2FSUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5PC57OTDuUU4> NXHp[lh5W0GQR1XS
human LOXIMVI cell NUPvRnJXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGxQYEmPVlmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFgvOzJibl2u M2DKbnNCVkeHUh?=
human D-336MG cell NF3SRVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFfVUYNKdmirYnn0bY9vKG:oIHj1cYFvKERvM{O2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PDZwMjDuUU4> M4j2c3NCVkeHUh?=
human S-117 cell M3fUcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWTJcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= NFXsS3VUSU6JRWK=
human D-247MG cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{H4XGlvcGmkaYTpc44hd2ZiaIXtZY4hTC1{NEfNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1QC53MjDuUU4> MYDTRW5ITVJ?
human TYK-nu cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlv5TY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u M1;tcHNCVkeHUh?=
human A498 cell NITPTm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NG\weYVKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= MXvTRW5ITVJ?
human HepG2 cells NVXz[GRRTnWwY4Tpc44h[XO|YYm= MVSzJIg> NVfUd|BjUW6qaXLpeIlwdiCxZjDHV2s{NWKndHGgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jd[4x2[2:|ZTDpcpRwKGeueXPv[4VvKGGodHXyJFMhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o MmTJNlIzPjFyMkO=
human BCPAP cell NH24cWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w MYLTRW5ITVJ?
human KYSE-180 cell MljPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{\NUWlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2xPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd|IN88UU4> NHvRbo9USU6JRWK=
human MIA-PaCa-2 cell MlS3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlfzTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55NjFOwG0v MVHTRW5ITVJ?
human HCC1395 cell M{fvdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF|OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc5KM7:TT6= MVTTRW5ITVJ?
human RS4-11 cell NWPYdldmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;lTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2KM7:TT6= NIPLPFVUSU6JRWK=
human NCI-H2122 cell NX;BVJhTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrDemFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMkig{txONg>? MX;TRW5ITVJ?
human SNU-423 cell NGTTenZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYPJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4Phfg+9lCCLQ{WwQVIvPSEQvF2u NVTSeFdYW0GQR1XS
human SK-LMS-1 cell NV\vT49IT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2LEcWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjZ2IN88UU4> NEWwbYJUSU6JRWK=
human RPMI-7951 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1Pj[WlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST23PVUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{Lkeg{txONg>? MWjTRW5ITVJ?
human COLO-829 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTUSIRRUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w M3\KN3NCVkeHUh?=
human SCC-9 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlLpTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= MoHBV2FPT0WU
human A704 cell NXTrb2hZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2L6c2lvcGmkaYTpc44hd2ZiaIXtZY4hSTdyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNFgyOiEQvF2u MoPOV2FPT0WU
human HOP-62 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlrBTY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlM3ODV2IN88UU4> NHjVV4hUSU6JRWK=
human HCC1569 cell NXfQU5JyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUDFeZJ7UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxOVY6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy52OEOwOUDPxE1w M1rmbHNCVkeHUh?=
human A172 cell NYexN5N7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M33HdmlvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|U1QThizszNMi=> NVjEPHNYW0GQR1XS
human MOLT-16 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3PsWmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDh3NU[g{txONg>? NXOzVHJDW0GQR1XS
human TE-15 cell MomxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPzS4JiUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTV|NEOg{txONg>? M3fCcnNCVkeHUh?=
human OE19 cell MojQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUXJcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= NHTUe2ZUSU6JRWK=
human MHH-ES-1 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xPDV2NTFOwG0v NH7sNJlUSU6JRWK=
human NKM-1 cell MmLIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIXmbGtKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v M4Ta[3NCVkeHUh?=
human RCC10RGB cell NH7WV41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHjrV4dKdmirYnn0bY9vKG:oIHj1cYFvKFKFQ{GwVmdDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5{OUS3PUDPxE1? M3[1NnNCVkeHUh?=
human BxPC-3 cell M4rzNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzJc5ZNUW6qaXLpeIlwdiCxZjDoeY1idiCEeGDDMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjdyM{mxJO69VS5? NXz4[XZNW0GQR1XS
human ALL-PO cell M4LFT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmfPTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{QDV6IN88UU4> M2n3WnNCVkeHUh?=
human SK-OV-3 cell M1LXUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIToT5NKdmirYnn0bY9vKG:oIHj1cYFvKFONLV;WMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl7M{Sg{txONg>? M17vb3NCVkeHUh?=
human SW1710 cell MoXzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXC[mpMUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjR{NEW2JO69VS5? NIrjVFlUSU6JRWK=

... Click to View More Cell Line Experimental Data

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]

+ 展开
  • 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]

+ 展开
  • 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
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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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GSK-3 Signaling Pathway Map

GSK-3 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID