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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Choose Selective GSK-3 Inhibitors

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 M2f0XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvpV2xKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> M3vOd3NCVkeHUh?=
human GCT cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTEW2ZiUW6qaXLpeIlwdiCxZjDoeY1idiCJQ2SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFYvPzJibl2u MkWwV2FPT0WU
human 769-P cell NYXNbmc4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\2cWlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFQvQTlibl2u MX\TRW5ITVJ?
human LOXIMVI cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljKTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> MYjTRW5ITVJ?
human D-336MG cell NX70SVE2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVzOWm5UUW6qaXLpeIlwdiCxZjDoeY1idiCGLUOzOm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDR4LkKgcm0v NI\UdW1USU6JRWK=
human S-117 cell NFLLelRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1O2SGlvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25NlEvOzFibl2u MWTTRW5ITVJ?
human D-247MG cell NYTadnltT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1zCNmlvcGmkaYTpc44hd2ZiaIXtZY4hTC1{NEfNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1QC53MjDuUU4> NVfLU5JGW0GQR1XS
human TYK-nu cell NHrSOFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkfQTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u MWLTRW5ITVJ?
human A498 cell M2fXfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYOwR45zUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{KM7:TT6= NHfncIFUSU6JRWK=
human HepG2 cells Ml[0SpVv[3Srb36gZZN{[Xl? MVqzJIg> M3\1NmlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXXfseYNwe2ViaX70c{BodHmlb3flckBi\nSncjCzJIhzeyCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[y=> MU[yNlI3OTB{Mx?=
human BCPAP cell MmLtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4H4dWlvcGmkaYTpc44hd2ZiaIXtZY4hSkOSQWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY4KM7:TT6= MUfTRW5ITVJ?
human KYSE-180 cell Mmf3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HoS2lvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2xPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd|IN88UU4> M3rsVnNCVkeHUh?=
human MIA-PaCa-2 cell NYjUbW1LT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd4IN88UU4> NX;2dIhWW0GQR1XS
human HCC1395 cell MoTMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGjyUnVKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{GzPVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd6IN88UU4> Mn3yV2FPT0WU
human RS4-11 cell NYjISXJmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVUh|ryPLh?= MnzhV2FPT0WU
human NCI-H2122 cell M361eGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUDJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvOjhizszNMi=> M3\WenNCVkeHUh?=
human SNU-423 cell NYjTdpg4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4Phfg+9lCCLQ{WwQVIvPSEQvF2u NIXqXphUSU6JRWK=
human SK-LMS-1 cell MlfrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUjyenFGUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwNkSg{txONg>? NFTNOpJUSU6JRWK=
human RPMI-7951 cell NEnUSm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;U[ZFKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? MXPTRW5ITVJ?
human COLO-829 cell NHPSPHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV;VWXNRUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w NVy4bWxQW0GQR1XS
human SCC-9 cell NVXJW|ZMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUG3SHNyUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTVizszNMi=> NX2xOY1kW0GQR1XS
human A704 cell M{DtdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGTXOG9KdmirYnn0bY9vKG:oIHj1cYFvKEF5MESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlA5OTJizszNMi=> NWHCfFNJW0GQR1XS
human HOP-62 cell M1\U[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4C5XmlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{PjB3NDFOwG0v NHjQOm9USU6JRWK=
human HCC1569 cell M2DybGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXTJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF3NkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OzB3IN88UU4> MnW3V2FPT0WU
human A172 cell MkXsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HrRmlvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|U1QThizszNMi=> NU\xfnpXW0GQR1XS
human MOLT-16 cell NFzPcFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIrNW5BKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh6NUW2JO69VS5? MUPTRW5ITVJ?
human TE-15 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MorGTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVU{PDNizszNMi=> MmfjV2FPT0WU
human OE19 cell NWfJcFRoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjVboVmUW6qaXLpeIlwdiCxZjDoeY1idiCRRUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PjR3MTFOwG0v NXi4TlFFW0GQR1XS
human MHH-ES-1 cell MmL3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUDwdm9xUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMES1OFUh|ryPLh?= MYjTRW5ITVJ?
human NKM-1 cell NGPNOlNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGXWSmdKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v M1qzbHNCVkeHUh?=
human RCC10RGB cell NFf4XmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoW2TY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO M{\LeXNCVkeHUh?=
human BxPC-3 cell NWjZ[Gd1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4jreWlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44ODN7MTFOwG0v MnXhV2FPT0WU
human ALL-PO cell M3T0R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\iTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{QDV6IN88UU4> NXmxfZNSW0GQR1XS
human SK-OV-3 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk6OzRizszNMi=> NFfsXoNUSU6JRWK=
human SW1710 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn7JTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQzPDV4IN88UU4> Mn\sV2FPT0WU

... 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(Data is from Selleck tests instead of citations):
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