CHIR-99021 (CT99021)

For research use only.

Catalog No.S1263

390 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. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

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Selleck's CHIR-99021 (CT99021) has been cited by 390 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. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
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 NFLxcHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYXIR2E4UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC5zNjDuUU4> MWfTRW5ITVJ?
human GCT cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGdEXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNyNj63NkBvVS5? MoLCV2FPT0WU
human 769-P cell NY\USpFvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUn1RmpRUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5PC57OTDuUU4> NX33XZg{W0GQR1XS
human LOXIMVI cell MkOwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NED4WGlKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02QDhwM{Kgcm0v M1\QSXNCVkeHUh?=
human D-336MG cell NXfROHBTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYfz[4lwUW6qaXLpeIlwdiCxZjDoeY1idiCGLUOzOm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDR4LkKgcm0v NV7iW|NEW0GQR1XS
human S-117 cell MnXxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI\wXVlKdmirYnn0bY9vKG:oIHj1cYFvKFNvMUG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIyNjNzIH7NMi=> M1nyd3NCVkeHUh?=
human D-247MG cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LOZmlvcGmkaYTpc44hd2ZiaIXtZY4hTC1{NEfNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1QC53MjDuUU4> MX\TRW5ITVJ?
human TYK-nu cell NWLhfYRuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2foSWlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xPzlizszNMi=> M{ToOnNCVkeHUh?=
human A498 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV\U[mhkUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{KM7:TT6= MX3TRW5ITVJ?
human HepG2 cells MYDGeY5kfGmxbjDhd5NigQ>? MWKzJIg> MkPrTY5pcWKrdHnvckBw\iCJU1uzMYJmfGFiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lb4Lwc5JifGmxbjDv[kBcO0ifZ3z1Z49{\SCrboTvJIdtgWOxZ3XuJIFnfGW{IEOgbJJ{KGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7n M4SwXlIzOjZzMEKz
human BCPAP cell NUC1NplOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXfJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w NFvDPGtUSU6JRWK=
human KYSE-180 cell NYntXoFsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTqTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> M3jvNXNCVkeHUh?=
human MIA-PaCa-2 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHXnbI9KdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke2JO69VS5? MYLTRW5ITVJ?
human HCC1395 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnHzTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44QCEQvF2u M4Tne3NCVkeHUh?=
human RS4-11 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGX6[|RKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTVizszNMi=> NHfUN5hUSU6JRWK=
human NCI-H2122 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{XNbWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{ODFOwG0v M1TSb3NCVkeHUh?=
human SNU-423 cell NUTNdINyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\xWmlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi53IN88UU4> NGDYWmhUSU6JRWK=
human SK-LMS-1 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHlNXZbUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwNkSg{txONg>? Ml3uV2FPT0WU
human RPMI-7951 cell Mm\aS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVm2SlltUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVc6PTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3Ojef-8kEBKSzVyPUKuO{DPxE1w MYnTRW5ITVJ?
human COLO-829 cell NEO5[pRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVzDPGN1UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w MoOzV2FPT0WU
human SCC-9 cell MoexS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnTnTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= MmTOV2FPT0WU
human A704 cell M4XMfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJGE4ODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVIh|ryPLh?= MV7TRW5ITVJ?
human HOP-62 cell NEmzZYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXaS3RUUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjN4MEW0JO69VS5? MXPTRW5ITVJ?
human HCC1569 cell Mo\xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoLiTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNU[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDNyNTFOwG0v NYPpeVFSW0GQR1XS
human A172 cell NUjQT|RyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGEyPzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lke1OFk5KM7:TT6= MVzTRW5ITVJ?
human MOLT-16 cell MmrGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg5PTV4IN88UU4> NUTVU|A3W0GQR1XS
human TE-15 cell MnrKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\0TY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVU{PDNizszNMi=> MnOyV2FPT0WU
human OE19 cell M1TuRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXvJcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= NWPxWHE6W0GQR1XS
human MHH-ES-1 cell M1rWT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;LOnFKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yNEW0OUDPxE1w M2LJWnNCVkeHUh?=
human NKM-1 cell M{DlW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HMW2lvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE{QTdzIN88UU4> MXXTRW5ITVJ?
human RCC10RGB cell NHrsWmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUW5OG1TUW6qaXLpeIlwdiCxZjDoeY1idiCUQ1OxNHJISiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMkm0O|kh|ryP NXixSmdqW0GQR1XS
human BxPC-3 cell Mn3DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3ziSWlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44ODN7MTFOwG0v M{HlcXNCVkeHUh?=
human ALL-PO cell NWjOSpB4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH7afFRKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDN6NUig{txONg>? M2nnZ3NCVkeHUh?=
human SK-OV-3 cell M1\ucmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mmm3TY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46QTN2IN88UU4> MVnTRW5ITVJ?
human SW1710 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVLJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuOFI1PTZizszNMi=> NHXXT3hUSU6JRWK=

... 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
  • 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=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID