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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Cited by 18 Publications

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.

Purity & Quality Control

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 MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVLyXmo{UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC5zNjDuUU4> NELIVoZUSU6JRWK=
human GCT cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHGXIM6UW6qaXLpeIlwdiCxZjDoeY1idiCJQ2SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFYvPzJibl2u NUXRWmNLW0GQR1XS
human 769-P cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3PlXmlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFQvQTlibl2u M37xdnNCVkeHUh?=
human LOXIMVI cell Ml7KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1PWPGlvcGmkaYTpc44hd2ZiaIXtZY4hVE:[SV3WTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5QC5|MjDuUU4> M1vkbHNCVkeHUh?=
human D-336MG cell NUnLc4NuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn;ITY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFQ3NjJibl2u NVLVeXp1W0GQR1XS
human S-117 cell NV\2Vpk1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TtTmlvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25NlEvOzFibl2u MkPKV2FPT0WU
human D-247MG cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofvTY5pcWKrdHnvckBw\iCqdX3hckBFNTJ2N13HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQ5NjV{IH7NMi=> Mln1V2FPT0WU
human TYK-nu cell NX7Eeo5MT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFc6KM7:TT6= MkWzV2FPT0WU
human A498 cell NUX2Xo9zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;LTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zJO69VS5? M2LGS3NCVkeHUh?=
human HepG2 cells MVHGeY5kfGmxbjDhd5NigQ>? MYWzJIg> NH[3ZmxKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> M{nXTVIzOjZzMEKz
human BCPAP cell M1q4cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHO4cIRKdmirYnn0bY9vKG:oIHj1cYFvKEKFUFHQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PyEQvF2u MYPTRW5ITVJ?
human KYSE-180 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mk\OTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> NFPlbYdUSU6JRWK=
human MIA-PaCa-2 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH7tXIlKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke2JO69VS5? NGW2ZmVUSU6JRWK=
human HCC1395 cell Mn7lS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFrsUY5KdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{GzPVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd6IN88UU4> NUjJb|JNW0GQR1XS
human RS4-11 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVe1eHk{UW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl3IN88UU4> MYXTRW5ITVJ?
human NCI-H2122 cell M2faSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHSTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxNlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjJ6IN88UU4> M4PzZXNCVkeHUh?=
human SNU-423 cell MlG2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHmTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0zNjVizszNMi=> NEDaUo9USU6JRWK=
human SK-LMS-1 cell NWm1VHk2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1zuSmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjZ2IN88UU4> M2jiTXNCVkeHUh?=
human RPMI-7951 cell NH\aelJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLPVo5KdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? MUjTRW5ITVJ?
human COLO-829 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWm2VVFyUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w NFTWXVNUSU6JRWK=
human SCC-9 cell NVfpd29zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHqz[IRKdmirYnn0bY9vKG:oIHj1cYFvKFOFQz25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46PSEQvF2u NEDyTFRUSU6JRWK=
human A704 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYLxNppwUW6qaXLpeIlwdiCxZjDoeY1idiCDN{C0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4xQDF{IN88UU4> M1TCWHNCVkeHUh?=
human HOP-62 cell NIL2S4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH\WSXhKdmirYnn0bY9vKG:oIHj1cYFvKEiRUD22NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOzZyNUSg{txONg>? MVjTRW5ITVJ?
human HCC1569 cell NGXYZnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2PYS2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUW2PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDh|MEWg{txONg>? M4rlTHNCVkeHUh?=
human A172 cell M2\wWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXP5bWFOUW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{44PTR7ODFOwG0v NWrWb5dPW0GQR1XS
human MOLT-16 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2fGemlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDh3NU[g{txONg>? Mof2V2FPT0WU
human TE-15 cell NGOzVGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HFcGlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> MVnTRW5ITVJ?
human OE19 cell NFrtOplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= M4\DZ3NCVkeHUh?=
human MHH-ES-1 cell NEfLd4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\hXW5sUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMES1OFUh|ryPLh?= M17vc3NCVkeHUh?=
human NKM-1 cell Ml;4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\DTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVM6PzFizszNMi=> MV;TRW5ITVJ?
human RCC10RGB cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWnZcYRSUW6qaXLpeIlwdiCxZjDoeY1idiCUQ1OxNHJISiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMkm0O|kh|ryP NXPEVYt7W0GQR1XS
human BxPC-3 cell Mo\oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|A{QTFizszNMi=> M1\ERnNCVkeHUh?=
human ALL-PO cell NFzu[HFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFXqSmFKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDN6NUig{txONg>? MoHrV2FPT0WU
human SK-OV-3 cell NFn2WWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fiTWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v NED3fWhUSU6JRWK=
human SW1710 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1vMXmlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41OjR3NjFOwG0v MWfTRW5ITVJ?

... 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