CHIR-99021 (CT99021)

Catalog No.S1263

CHIR-99021 (CT99021) Chemical Structure

Molecular Weight(MW): 465.34

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

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2 Customer Reviews

  • 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.

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Biological Activity

Description CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
In vitro

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 NHT2eJRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2fTcGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvOTZibl2u MUnTRW5ITVJ?
human GCT cell NICxNWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVXic5IxUW6qaXLpeIlwdiCxZjDoeY1idiCJQ2SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFYvPzJibl2u MlG5V2FPT0WU
human 769-P cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn\LTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW4OE46QSCwTT6= NX60eYtvW0GQR1XS
human LOXIMVI cell MkDmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk\UTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> NEn6XXVUSU6JRWK=
human D-336MG cell MlPLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1S3NWlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg1Pi5{IH7NMi=> MX\TRW5ITVJ?
human S-117 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn;ITY5pcWKrdHnvckBw\iCqdX3hckBUNTFzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmyNU4{OSCwTT6= Mn7yV2FPT0WU
human D-247MG cell M3T0d2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEjiRpVKdmirYnn0bY9vKG:oIHj1cYFvKERvMkS3UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PDhwNUKgcm0v MoLqV2FPT0WU
human TYK-nu cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUW3c4NKUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v M4nB[XNCVkeHUh?=
human A498 cell MmPiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOg{txONg>? Mo[wV2FPT0WU
human HepG2 cells NVu4S4JQTnWwY4Tpc44h[XO|YYm= M2PWflMhcA>? NEfHcm9KdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> MkC1NlIzPjFyMkO=
human BCPAP cell M3fIWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3yT4pbUW6qaXLpeIlwdiCxZjDoeY1idiCEQ2DBVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjdizszNMi=> MXrTRW5ITVJ?
human KYSE-180 cell M3[1[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVvJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44OyEQvF2u M2PJUHNCVkeHUh?=
human MIA-PaCa-2 cell NYC3UW5vT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoLTTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55NjFOwG0v NHrFXYlUSU6JRWK=
human HCC1395 cell NUnU[JkyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXLMbY4{UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxN|k2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55ODFOwG0v M2HBWXNCVkeHUh?=
human RS4-11 cell Ml33S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{PBWmlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u NHPYVWtUSU6JRWK=
human NCI-H2122 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYewV|JtUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4JO69VS5? MoDjV2FPT0WU
human SNU-423 cell NWLaPWVLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvQd2ZuUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{LkWg{txONg>? M3LUNHNCVkeHUh?=
human SK-LMS-1 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWnVTmE4UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwNkSg{txONg>? MU\TRW5ITVJ?
human RPMI-7951 cell NW\mOotyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;VPYlKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? MnT3V2FPT0WU
human COLO-829 cell MmXZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH25[JdKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFI6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi55NkW0JO69VS5? NF7PdVFUSU6JRWK=
human SCC-9 cell M2np[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXG2WWxnUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTVizszNMi=> M2i5enNCVkeHUh?=
human A704 cell M1q4XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVfRd5pmUW6qaXLpeIlwdiCxZjDoeY1idiCDN{C0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4xQDF{IN88UU4> NVnoRWdyW0GQR1XS
human HOP-62 cell M4LBRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJGhQWC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|YxPTRizszNMi=> M2W5VHNCVkeHUh?=
human HCC1569 cell NX;xb3ZwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXLJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF3NkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OzB3IN88UU4> M1izVnNCVkeHUh?=
human A172 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnHvTY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63OVQ6QCEQvF2u NUPSO41kW0GQR1XS
human MOLT-16 cell NIfE[WxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg5PTV4IN88UU4> MmHDV2FPT0WU
human TE-15 cell M3Xadmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4rzXWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> NHvGb|RUSU6JRWK=
human OE19 cell NEXPVpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlH2TY5pcWKrdHnvckBw\iCqdX3hckBQTTF7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OlQ2OSEQvF2u MYPTRW5ITVJ?
human MHH-ES-1 cell M3\Ofmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjRTY5pcWKrdHnvckBw\iCqdX3hckBOUEhvRWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODR3NEWg{txONg>? MXfTRW5ITVJ?
human NKM-1 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlv2TY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVM6PzFizszNMi=> NU\j[JZ2W0GQR1XS
human RCC10RGB cell MofpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk\CTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO MoW0V2FPT0WU
human BxPC-3 cell NX3NRWYyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mme0TY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlcxOzlzIN88UU4> M4nyWnNCVkeHUh?=
human ALL-PO cell NILoUHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NI[0NmdKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDN6NUig{txONg>? MkTZV2FPT0WU
human SK-OV-3 cell M{DIWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\Tc2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v MXfTRW5ITVJ?
human SW1710 cell M2jLXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYW3[pNbUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjR{NEW2JO69VS5? NGKyRVVUSU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo 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].

Protocol

Cell Research:

[1]

+ Expand
  • 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)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 10 mg/mL warmed (21.48 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
3.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 465.34
Formula

C22H18Cl2N8

CAS No. 252917-06-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID