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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1 Customer Review

  • 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.
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 Mmn5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\0TY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxOE4yPiCwTT6= MUXTRW5ITVJ?
human GCT cell NGr3[YNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml7qTY5pcWKrdHnvckBw\iCqdX3hckBIS1RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ME[uO|Ihdk1w NWW2[FNyW0GQR1XS
human 769-P cell Mny0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHe5OnFKdmirYnn0bY9vKG:oIHj1cYFvKDd4OT3QJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg1Njl7IH7NMi=> NGTsfXVUSU6JRWK=
human LOXIMVI cell NH7OU2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoTyTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> MVvTRW5ITVJ?
human D-336MG cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFPx[pRKdmirYnn0bY9vKG:oIHj1cYFvKERvM{O2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PDZwMjDuUU4> NXT3PWVYW0GQR1XS
human S-117 cell NWW5RYxJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\GTmdyUW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> MkT1V2FPT0WU
human D-247MG cell MlzGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\MTo5[UW6qaXLpeIlwdiCxZjDoeY1idiCGLUK0O21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTR6LkWyJI5ONg>? NVv3OIZZW0GQR1XS
human TYK-nu cell M37TOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXm3eoJJUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v Ml7GV2FPT0WU
human A498 cell NVnLSoRKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXHNSVY2UW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{KM7:TT6= M4noTHNCVkeHUh?=
human HepG2 cells M1rRSWZ2dmO2aX;uJIF{e2G7 M1TSbFMhcA>? M4fMTGlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXXfseYNwe2ViaX70c{BodHmlb3flckBi\nSncjCzJIhzeyCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[y=> M3TLZ|IzOjZzMEKz
human BCPAP cell M2nad2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDQTY5pcWKrdHnvckBw\iCqdX3hckBDS1CDUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlch|ryPLh?= NEDDbI1USU6JRWK=
human KYSE-180 cell Ml;4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44OyEQvF2u NXLtUIVqW0GQR1XS
human MIA-PaCa-2 cell NVfxbVBQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYjJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd4IN88UU4> NH3xPGdUSU6JRWK=
human HCC1395 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4fqS2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUO5OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzhizszNMi=> Mmm4V2FPT0WU
human RS4-11 cell NFnxRVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnq2TY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2KM7:TT6= MlXDV2FPT0WU
human NCI-H2122 cell NVS5[HlzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWL6RmJDUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4JO69VS5? MX3TRW5ITVJ?
human SNU-423 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfrTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0zNjVizszNMi=> M4nKRnNCVkeHUh?=
human SK-LMS-1 cell MnjIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVLpfIl7UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwNkSg{txONg>? MmC2V2FPT0WU
human RPMI-7951 cell MnrES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M17DbWlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST23PVUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{Lkeg{txONg>? M2CzWXNCVkeHUh?=
human COLO-829 cell NIjtNHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoH6TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUiyPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPzZ3NDFOwG0v NUPRWIp1W0GQR1XS
human SCC-9 cell M2nicWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNESy17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65OUDPxE1w MoPDV2FPT0WU
human A704 cell NFmzTYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1OyO2lvcGmkaYTpc44hd2ZiaIXtZY4hSTdyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNFgyOiEQvF2u NFz0[JNUSU6JRWK=
human HOP-62 cell NXPZ[HBWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGhQWC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|YxPTRizszNMi=> M{i4SXNCVkeHUh?=
human HCC1569 cell MnrWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{jlUmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUW2PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDh|MEWg{txONg>? M2ntN3NCVkeHUh?=
human A172 cell M3K4TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJGEyPzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lke1OFk5KM7:TT6= NIDaWlhUSU6JRWK=
human MOLT-16 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg5PTV4IN88UU4> NEDBTmtUSU6JRWK=
human TE-15 cell NImyTHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEnLNFRKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PTN2MzFOwG0v M4e5WHNCVkeHUh?=
human OE19 cell NGiw[4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUHJcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= MV\TRW5ITVJ?
human MHH-ES-1 cell NX\uSXFyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrSXHhKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yNEW0OUDPxE1w M3rWVHNCVkeHUh?=
human NKM-1 cell MnTNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\kNmlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE{QTdzIN88UU4> M3;wXnNCVkeHUh?=
human RCC10RGB cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoHhTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO M{X0UXNCVkeHUh?=
human BxPC-3 cell NED2OpFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHL4VpRKdmirYnn0bY9vKG:oIHj1cYFvKEK6UFOtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzB|OUGg{txONg>? MYDTRW5ITVJ?
human ALL-PO cell NFG3UGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkHKTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{QDV6IN88UU4> Mmi2V2FPT0WU
human SK-OV-3 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFzNflRKdmirYnn0bY9vKG:oIHj1cYFvKFONLV;WMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl7M{Sg{txONg>? NXvwdlJzW0GQR1XS
human SW1710 cell M4HMb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF7ufpJKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? NX71O5NLW0GQR1XS

... 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].


Cell Research:


+ 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:


+ 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.

* 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


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID