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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  • 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.

Purity & Quality Control

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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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] GSK-3α [1]
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 NHTRfVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnjeGx{UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC5zNjDuUU4> MYLTRW5ITVJ?
human GCT cell MmrsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M121cmlvcGmkaYTpc44hd2ZiaIXtZY4hT0OWIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{C2MlczKG6PLh?= MUDTRW5ITVJ?
human 769-P cell NFLpT|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rQeGlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFQvQTlibl2u Mnu4V2FPT0WU
human LOXIMVI cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEf0ZldKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02QDhwM{Kgcm0v NYPQbYdFW0GQR1XS
human D-336MG cell M2Xm[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHBWmJ2UW6qaXLpeIlwdiCxZjDoeY1idiCGLUOzOm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDR4LkKgcm0v Mly2V2FPT0WU
human S-117 cell NHftWJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXHNOZplUW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> MYjTRW5ITVJ?
human D-247MG cell NFP2TFNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXW5[GpKUW6qaXLpeIlwdiCxZjDoeY1idiCGLUK0O21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTR6LkWyJI5ONg>? MXLTRW5ITVJ?
human TYK-nu cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXZTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u MYHTRW5ITVJ?
human A498 cell MnrjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF21R|RKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= NXT1[WlpW0GQR1XS
human HepG2 cells MXLGeY5kfGmxbjDhd5NigQ>? M3y0NFMhcA>? NHjpSIRKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> NHjjfGMzOjJ4MUCyNy=>
human BCPAP cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlfpTY5pcWKrdHnvckBw\iCqdX3hckBDS1CDUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlch|ryPLh?= MmTHV2FPT0WU
human KYSE-180 cell MlLBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33uVmlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2xPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd|IN88UU4> MUDTRW5ITVJ?
human MIA-PaCa-2 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF[3OmNKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke2JO69VS5? MUfTRW5ITVJ?
human HCC1395 cell M{WybGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHP0UHZKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{GzPVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd6IN88UU4> NFTpZ2FUSU6JRWK=
human RS4-11 cell NXm5RWpjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4[2XGlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u NIHYdZRUSU6JRWK=
human NCI-H2122 cell NHXaO4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mk[zTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxNlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjJ6IN88UU4> NE\FZpNUSU6JRWK=
human SNU-423 cell NWrq[WN[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnacXZKUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{LkWg{txONg>? M3zJV3NCVkeHUh?=
human SK-LMS-1 cell MmPKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TrXGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjZ2IN88UU4> M2n1ZXNCVkeHUh?=
human RPMI-7951 cell NEHNdWNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnWwTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNzFOwG0v NH7ub5VUSU6JRWK=
human COLO-829 cell M4j1dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NY\oV2kyUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w NWfJbYJXW0GQR1XS
human SCC-9 cell NHfMUYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1PITGlvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlk2KM7:TT6= NWnZXpB2W0GQR1XS
human A704 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGE4ODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVIh|ryPLh?= Mmq1V2FPT0WU
human HOP-62 cell NYjhc41VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVLycnlDUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjN4MEW0JO69VS5? MkLFV2FPT0WU
human HCC1569 cell NY\CUoVST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF3NkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OzB3IN88UU4> MYPTRW5ITVJ?
human A172 cell NInlbVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTJO2FKdmirYnn0bY9vKG:oIHj1cYFvKEFzN{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlc2PDl6IN88UU4> M4HO[HNCVkeHUh?=
human MOLT-16 cell M1jKcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg5PTV4IN88UU4> MUHTRW5ITVJ?
human TE-15 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3PzSmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> NIPKSFlUSU6JRWK=
human OE19 cell NGSxUoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVrnR4o6UW6qaXLpeIlwdiCxZjDoeY1idiCRRUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PjR3MTFOwG0v MmDlV2FPT0WU
human MHH-ES-1 cell M4Hk[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFzzdJpKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yNEW0OUDPxE1w MnLLV2FPT0WU
human NKM-1 cell NITuOYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGnZW4FKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v NFvweIhUSU6JRWK=
human RCC10RGB cell M{HCSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4DOTmlvcGmkaYTpc44hd2ZiaIXtZY4hWkOFMUDSS2Ih[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjJ7NEe5JO69VQ>? MkX0V2FPT0WU
human BxPC-3 cell NFr5NlVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmPDTY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlcxOzlzIN88UU4> MV3TRW5ITVJ?
human ALL-PO cell NIf6b|lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFM5PThizszNMi=> NFSwcGpUSU6JRWK=
human SK-OV-3 cell Mo\6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XvSGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v NH7EdHNUSU6JRWK=
human SW1710 cell MmnJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrTZnZKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? M4\tTnNCVkeHUh?=

... 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 78 mg/mL warmed (167.61 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 3.5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID