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.
Targets
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 MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGTIeHdKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> M3fHXnNCVkeHUh?=
human GCT cell NHrnVWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUOx[YFUUW6qaXLpeIlwdiCxZjDoeY1idiCJQ2SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFYvPzJibl2u MlqyV2FPT0WU
human 769-P cell NX\zZmFuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mli3TY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW4OE46QSCwTT6= M2HuW3NCVkeHUh?=
human LOXIMVI cell NGPlVo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MofRTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> MkKzV2FPT0WU
human D-336MG cell MofVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3qxUmlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg1Pi5{IH7NMi=> NWruXIVFW0GQR1XS
human S-117 cell MmDRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn[wTY5pcWKrdHnvckBw\iCqdX3hckBUNTFzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmyNU4{OSCwTT6= MUPTRW5ITVJ?
human D-247MG cell NEPkWYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWri[I5IUW6qaXLpeIlwdiCxZjDoeY1idiCGLUK0O21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTR6LkWyJI5ONg>? M2DMR3NCVkeHUh?=
human TYK-nu cell NG\LOndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUXz[YNzUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v MlvrV2FPT0WU
human A498 cell NWDVWXZFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGWxWoZKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= NUX4d4hPW0GQR1XS
human HepG2 cells MV7GeY5kfGmxbjDhd5NigQ>? M1PqV|MhcA>? M3LqV2lvcGmkaYTpc44hd2ZiR2PLN{1j\XSjIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXXfseYNwe2ViaX70c{BodHmlb3flckBi\nSncjCzJIhzeyCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[y=> NIrjS|IzOjJ4MUCyNy=>
human BCPAP cell MmX2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFrFVpRKdmirYnn0bY9vKG:oIHj1cYFvKEKFUFHQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PyEQvF2u NUjjPVFVW0GQR1XS
human KYSE-180 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44OyEQvF2u MWHTRW5ITVJ?
human MIA-PaCa-2 cell M1mwPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nBVWlvcGmkaYTpc44hd2ZiaIXtZY4hVUmDLWDhR4EuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwN{[g{txONg>? Mn;4V2FPT0WU
human HCC1395 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NELmZmxKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{GzPVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd6IN88UU4> Mmf2V2FPT0WU
human RS4-11 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2eyWGlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u M{XyeHNCVkeHUh?=
human NCI-H2122 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4KyTWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{ODFOwG0v NHTGdpdUSU6JRWK=
human SNU-423 cell M1XhUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIXkOIxKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNTFOwG0v MmLMV2FPT0WU
human SK-LMS-1 cell NGLZWIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\sTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPjRizszNMi=> NXXyU|N4W0GQR1XS
human RPMI-7951 cell NIfJflRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWLVOHR5UW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVc6PTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3Ojef-8kEBKSzVyPUKuO{DPxE1w NYCzRWF5W0GQR1XS
human COLO-829 cell NE\3WW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrEUFZKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFI6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi55NkW0JO69VS5? M3n0bnNCVkeHUh?=
human SCC-9 cell NVLy[JBbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\kWGlvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlk2KM7:TT6= MlvyV2FPT0WU
human A704 cell NV\3TZJtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUHNOpZPUW6qaXLpeIlwdiCxZjDoeY1idiCDN{C0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4xQDF{IN88UU4> NGXmbWxUSU6JRWK=
human HOP-62 cell NEXtVnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGhQWC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|YxPTRizszNMi=> M4CwcHNCVkeHUh?=
human HCC1569 cell M2PUdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXDc5V7UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxOVY6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy52OEOwOUDPxE1w NHfj[2NUSU6JRWK=
human A172 cell NVzTSVJVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1juWmlvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|U1QThizszNMi=> NXLzS5VTW0GQR1XS
human MOLT-16 cell NXnp[Wd6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV3mWZJ3UW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy56OEW1OkDPxE1w M3PWfXNCVkeHUh?=
human TE-15 cell NIXUNHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4W5OWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> M1TwWHNCVkeHUh?=
human OE19 cell M3frO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVv4Rm9YUW6qaXLpeIlwdiCxZjDoeY1idiCRRUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PjR3MTFOwG0v M1TQTnNCVkeHUh?=
human MHH-ES-1 cell NHq1NIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX7pWYtVUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMES1OFUh|ryPLh?= M3PrUHNCVkeHUh?=
human NKM-1 cell MoHDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2\rfGlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE{QTdzIN88UU4> M{K5NHNCVkeHUh?=
human RCC10RGB cell M3S1XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnLqTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO M{T4e3NCVkeHUh?=
human BxPC-3 cell M4rZUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEeyO2lKdmirYnn0bY9vKG:oIHj1cYFvKEK6UFOtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzB|OUGg{txONg>? NFq3W|JUSU6JRWK=
human ALL-PO cell MmDHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1mwSGlvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45Ozh3ODFOwG0v M4TH[HNCVkeHUh?=
human SK-OV-3 cell MnfGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlTnTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46QTN2IN88UU4> NF20XlJUSU6JRWK=
human SW1710 cell M{PFRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\6OFRKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? M3;oU3NCVkeHUh?=

... 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 78 mg/mL warmed (167.61 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+ddH2O
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