CHIR-99021 (CT99021)

For research use only. Not for use in humans.

Catalog No.S1263

322 publications

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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Selleck's CHIR-99021 (CT99021) has been cited by 322 publications

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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]
(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 NGTVUmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE3KG6PLh?= MmH5V2FPT0WU
human GCT cell M{\RXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkT2TY5pcWKrdHnvckBw\iCqdX3hckBIS1RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ME[uO|Ihdk1w NX\T[JduW0GQR1XS
human 769-P cell M{PyS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nTSmlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFQvQTlibl2u MknoV2FPT0WU
human LOXIMVI cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGxQYEmPVlmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFgvOzJibl2u NUXXfIlDW0GQR1XS
human D-336MG cell MknMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OFYvOiCwTT6= MUjTRW5ITVJ?
human S-117 cell NIfaOoNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUTxSYhnUW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> M33RUnNCVkeHUh?=
human D-247MG cell NX7qbGFwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3vLUWlvcGmkaYTpc44hd2ZiaIXtZY4hTC1{NEfNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1QC53MjDuUU4> NUjBZ4lpW0GQR1XS
human TYK-nu cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUfmT|J5UW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v MojtV2FPT0WU
human A498 cell NEnTdpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXaN3BKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= NH\FeWhUSU6JRWK=
human HepG2 cells MlfJSpVv[3Srb36gZZN{[Xl? NX7sV4pXOyCq MVvJcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmOxcoDvdoF1cW:wIH;mJHs{UF2pbIXjc5NmKGmwdH:g[4x6[2:pZX6gZYZ1\XJiMzDodpMh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbne= NYPpeFhmOjJ{NkGwNlM>
human BCPAP cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7ON4RKdmirYnn0bY9vKG:oIHj1cYFvKEKFUFHQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PyEQvF2u M{e5ZnNCVkeHUh?=
human KYSE-180 cell MkjLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoGxTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> Mn\6V2FPT0WU
human MIA-PaCa-2 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3r0WWlvcGmkaYTpc44hd2ZiaIXtZY4hVUmDLWDhR4EuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwN{[g{txONg>? MojtV2FPT0WU
human HCC1395 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3nQOGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUO5OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzhizszNMi=> Mn:xV2FPT0WU
human RS4-11 cell M3\VTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFv6OJpKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTVizszNMi=> Mnn4V2FPT0WU
human NCI-H2122 cell NGX0XnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXrvTXN4UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4JO69VS5? MX3TRW5ITVJ?
human SNU-423 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkLVTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0zNjVizszNMi=> MUDTRW5ITVJ?
human SK-LMS-1 cell NFXPWFJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43PCEQvF2u NHu3O|dUSU6JRWK=
human RPMI-7951 cell MlTMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvN{m1NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi55IN88UU4> MWHTRW5ITVJ?
human COLO-829 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOEK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk44PjV2IN88UU4> NWGyTWpEW0GQR1XS
human SCC-9 cell NELCbWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjGW3ZbUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTVizszNMi=> MmnYV2FPT0WU
human A704 cell NX3L[3ltT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF2ySnBKdmirYnn0bY9vKG:oIHj1cYFvKEF5MESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlA5OTJizszNMi=> M4L4SHNCVkeHUh?=
human HOP-62 cell NHy5SJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnu0TY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlM3ODV2IN88UU4> NWjwfZV2W0GQR1XS
human HCC1569 cell MlLYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF3NkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OzB3IN88UU4> NGHiU4lUSU6JRWK=
human A172 cell M1;hOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{Dhe2lvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|U1QThizszNMi=> M2rZR3NCVkeHUh?=
human MOLT-16 cell M1HjfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVvJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg5PTV4IN88UU4> MmqxV2FPT0WU
human TE-15 cell M3jWXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYqxN2lmUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTV|NEOg{txONg>? MoD4V2FPT0WU
human OE19 cell NVO3PFlrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{LYTWlvcGmkaYTpc44hd2ZiaIXtZY4hV0VzOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVY1PTFizszNMi=> M3rKWnNCVkeHUh?=
human MHH-ES-1 cell MnHIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVXrXG5pUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMES1OFUh|ryPLh?= NF7EWXFUSU6JRWK=
human NKM-1 cell MmrhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEfTZm9KdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v NWD1OopqW0GQR1XS
human RCC10RGB cell NFW3XVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJHJESzFyUlfCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4zQTR5OTFOwG0> MnL2V2FPT0WU
human BxPC-3 cell M2HSRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrJTZVKdmirYnn0bY9vKG:oIHj1cYFvKEK6UFOtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzB|OUGg{txONg>? NYDTNXdvW0GQR1XS
human ALL-PO cell M2fWcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3vo[2lvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45Ozh3ODFOwG0v MXjTRW5ITVJ?
human SK-OV-3 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2O2ZWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v NYi5T|lpW0GQR1XS
human SW1710 cell M4fxU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHzSSWxKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? MVLTRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; 

PubMed: 30709379     


NCI-H460 cells were co-cultured with HUVECs in a 3D culture system, and then treated with 1 μM CHIR-99021, 10 μM or 20 μM Cisplatin, or a combination of both, for 24 h. Cells were harvested and immunoblotted with anti-cleaved PARP, anti-CD31, anti-VE-cadherin, anti-α-SMA, anti-vimentin, and anti-β-actin antibodies. 

CTNNB1; 

PubMed: 23993102     


Treatment with the GSK3β inhibitor CHIR-99021 led to increased levels of β-catenin in RKO and HT29 (non-mutant) cells.

β-catenin; 

PubMed: 24165128     


HeLa cells were treated with 5 μm CHIR-99021 for the indicated times. The samples were analyzed by Western blot.

30709379 23993102 24165128
Growth inhibition assay
Cell viability; 

PubMed: 22039301     


HMC-1.2 cells were cultured in the absence or presence of GSK3β inhibitor (CHIR 99021, 3-30 µM) and viability cell count was assessed by trypan blue dye exclusion after 24 h, 48 h or 72 h. All data are presented as the mean ± SEM of three independent experiments conducted in triplicate. p < 0.05*, p < 0.001** p < 0.0001*** vs vehicle treated control cells.

22039301
Immunofluorescence
SOX10/EdU; 

PubMed: 28174705     


Incorporation of EdU (white arrowheads) into SOX10+ ENS (enteric nervous system) cells with and without CHIR-99021.

Oct3/4; 

PubMed: 24779365     


Fluorescence micrographs showing the protein expression of Brachyury/Oct3/4 after a three day differentiation of ES-D3 cells with BIO (0.5 μM), SB-216763 (5 μM), CHIR-99021 (5 μM), or CHIR-98014 (1 μM). Nuclei were counterstained with DAPI (blue). The merge is shown in yellow. Original magnification 400x. Scale bar = 50 μm.

28174705 24779365
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]

- Collapse
  • 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]

- Collapse
  • 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
Smiles CC1=C[NH]C(=N1)C2=CN=C(NCCNC3=CC=C(C=N3)C#N)N=C2C4=CC=C(Cl)C=C4Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID