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 NGjm[YFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE3KG6PLh?= M{jXO3NCVkeHUh?=
human GCT cell Ml\ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEfmcVRKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwOk44OiCwTT6= M{nkbHNCVkeHUh?=
human 769-P cell M4L1emdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGHLe41KdmirYnn0bY9vKG:oIHj1cYFvKDd4OT3QJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg1Njl7IH7NMi=> NWDDRlh7W0GQR1XS
human LOXIMVI cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXTJcohq[mm2aX;uJI9nKGi3bXHuJGxQYEmPVlmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFgvOzJibl2u NULnXIVmW0GQR1XS
human D-336MG cell MoH1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVLkSXZYUW6qaXLpeIlwdiCxZjDoeY1idiCGLUOzOm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDR4LkKgcm0v NVnM[G1DW0GQR1XS
human S-117 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mke3TY5pcWKrdHnvckBw\iCqdX3hckBUNTFzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmyNU4{OSCwTT6= MnvyV2FPT0WU
human D-247MG cell M3:2ZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUmwRYZEUW6qaXLpeIlwdiCxZjDoeY1idiCGLUK0O21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTR6LkWyJI5ONg>? MWfTRW5ITVJ?
human TYK-nu cell NUK4dXpST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkniTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u MofJV2FPT0WU
human A498 cell MlLRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13sNGlvcGmkaYTpc44hd2ZiaIXtZY4hSTR7ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN{DPxE1w NGjGXYVUSU6JRWK=
human HepG2 cells MoDLSpVv[3Srb36gZZN{[Xl? NVHofYVrOyCq M3rqdGlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXXfseYNwe2ViaX70c{BodHmlb3flckBi\nSncjCzJIhzeyCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[y=> Mn\RNlIzPjFyMkO=
human BCPAP cell MlOwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w Ml\LV2FPT0WU
human KYSE-180 cell NIPLXZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\JTHlxUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVE5OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwN{Og{txONg>? MWfTRW5ITVJ?
human MIA-PaCa-2 cell NG[5cGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXThTlNRUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OkDPxE1w MoPmV2FPT0WU
human HCC1395 cell Mn\NS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLyTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44QCEQvF2u MYfTRW5ITVJ?
human RS4-11 cell NXfQUY1uT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn\TTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2KM7:TT6= M3PhNXNCVkeHUh?=
human NCI-H2122 cell M1zDOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fndWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{ODFOwG0v MlnVV2FPT0WU
human SNU-423 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX\h[WU{UW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{LkWg{txONg>? M1jHOHNCVkeHUh?=
human SK-LMS-1 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn;KTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPjRizszNMi=> NV3Kc4lvW0GQR1XS
human RPMI-7951 cell Ml3yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELKV4NKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? NUfuW4I4W0GQR1XS
human COLO-829 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXvGOmFCUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w MV3TRW5ITVJ?
human SCC-9 cell MlvSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmG1TY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= NXjOW4I1W0GQR1XS
human A704 cell Mn24S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13X[mlvcGmkaYTpc44hd2ZiaIXtZY4hSTdyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNFgyOiEQvF2u M2iyZnNCVkeHUh?=
human HOP-62 cell NVTMZXo6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3PWRmlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{PjB3NDFOwG0v MV3TRW5ITVJ?
human HCC1569 cell NWHafYlNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmfwTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNU[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDNyNTFOwG0v NFnzbHFUSU6JRWK=
human A172 cell NE\J[IRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoLoTY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63OVQ6QCEQvF2u NFKzRYJUSU6JRWK=
human MOLT-16 cell M{DGT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\XeGlJUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy56OEW1OkDPxE1w NWPVNWVzW0GQR1XS
human TE-15 cell NUezdYduT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mnm4TY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVU{PDNizszNMi=> NFXnb3hUSU6JRWK=
human OE19 cell M2PzVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnPqTY5pcWKrdHnvckBw\iCqdX3hckBQTTF7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OlQ2OSEQvF2u MnjjV2FPT0WU
human MHH-ES-1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfJNldKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yNEW0OUDPxE1w MWTTRW5ITVJ?
human NKM-1 cell M3H1O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI[wc29KdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v MnWxV2FPT0WU
human RCC10RGB cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJHJESzFyUlfCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4zQTR5OTFOwG0> NXL6U5JoW0GQR1XS
human BxPC-3 cell NFHPR3FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnQTY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlcxOzlzIN88UU4> MmXhV2FPT0WU
human ALL-PO cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUDJcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFM5PThizszNMi=> MUTTRW5ITVJ?
human SK-OV-3 cell M{Lmb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGrLUGJKdmirYnn0bY9vKG:oIHj1cYFvKFONLV;WMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl7M{Sg{txONg>? MljsV2FPT0WU
human SW1710 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFL2UY9KdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? MkfOV2FPT0WU

... 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 individually and in order:
4% DMSO+30% PEG 300+ddH2O

* 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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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