CHIR-99021 (CT99021)

For research use only.

Catalog No.S1263

366 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 366 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 MnPvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETwRnNKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> M3rmdHNCVkeHUh?=
human GCT cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGdEXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNyNj63NkBvVS5? MVvTRW5ITVJ?
human 769-P cell NHvSWHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoXnTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW4OE46QSCwTT6= Mn3iV2FPT0WU
human LOXIMVI cell M3z5dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFnzUlVKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02QDhwM{Kgcm0v NVLiVlloW0GQR1XS
human D-336MG cell MlK2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVjiUndbUW6qaXLpeIlwdiCxZjDoeY1idiCGLUOzOm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDR4LkKgcm0v MmfPV2FPT0WU
human S-117 cell M4HMS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= MkjPV2FPT0WU
human D-247MG cell M4DEdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnGU3F4UW6qaXLpeIlwdiCxZjDoeY1idiCGLUK0O21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTR6LkWyJI5ONg>? MkG0V2FPT0WU
human TYK-nu cell M1z6dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnziTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u M3XZRXNCVkeHUh?=
human A498 cell MkDiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGT5cVJKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= NVr4bVd1W0GQR1XS
human HepG2 cells MX3GeY5kfGmxbjDhd5NigQ>? NU\U[Y9ROyCq NF\hToJKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> MVeyNlI3OTB{Mx?=
human BCPAP cell M3X2NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w NUHRfFJ3W0GQR1XS
human KYSE-180 cell MkPBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVrjT5lrUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVE5OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwN{Og{txONg>? NHPhd2lUSU6JRWK=
human MIA-PaCa-2 cell NYXCbIZYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd4IN88UU4> M4XsenNCVkeHUh?=
human HCC1395 cell M4jsRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmmxTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44QCEQvF2u M1\PZnNCVkeHUh?=
human RS4-11 cell NX7hXmlvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYLJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVUh|ryPLh?= MlG0V2FPT0WU
human NCI-H2122 cell M3zCO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmnMTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxNlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjJ6IN88UU4> Mo[0V2FPT0WU
human SNU-423 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4q2WmlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi53IN88UU4> NXzQOItpW0GQR1XS
human SK-LMS-1 cell MoTBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43PCEQvF2u Moi2V2FPT0WU
human RPMI-7951 cell NGj5TZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEfoVVBKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? M1n2fHNCVkeHUh?=
human COLO-829 cell NUj5bVhST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\DSZZzUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w MWnTRW5ITVJ?
human SCC-9 cell NFH0XYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV3mZ4NVUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTVizszNMi=> MmDQV2FPT0WU
human A704 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{G3fmlvcGmkaYTpc44hd2ZiaIXtZY4hSTdyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNFgyOiEQvF2u M1:wenNCVkeHUh?=
human HOP-62 cell Mm\0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXjDSlZoUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjN4MEW0JO69VS5? NUO4[FF2W0GQR1XS
human HCC1569 cell NX;5W2FnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\ETY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNU[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDNyNTFOwG0v M{izbXNCVkeHUh?=
human A172 cell NXqzboxCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYDWSZBUUW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{44PTR7ODFOwG0v NX3GfZdNW0GQR1XS
human MOLT-16 cell NV3GV2x[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mny5TY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45QDV3NjFOwG0v NYXVfFZxW0GQR1XS
human TE-15 cell M{TiOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFv0TYZKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PTN2MzFOwG0v Ml63V2FPT0WU
human OE19 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mmq0TY5pcWKrdHnvckBw\iCqdX3hckBQTTF7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OlQ2OSEQvF2u MmnGV2FPT0WU
human MHH-ES-1 cell NEnBR3VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xPDV2NTFOwG0v MYfTRW5ITVJ?
human NKM-1 cell M3LibGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2CxUmlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE{QTdzIN88UU4> M2\acXNCVkeHUh?=
human RCC10RGB cell Mne1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn7zTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO MmnVV2FPT0WU
human BxPC-3 cell NU\qe4dZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWHBTXBUUW6qaXLpeIlwdiCxZjDoeY1idiCEeGDDMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjdyM{mxJO69VS5? M3jxV3NCVkeHUh?=
human ALL-PO cell NUnXbYF3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjndnBKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDN6NUig{txONg>? NYHSTYtIW0GQR1XS
human SK-OV-3 cell Mmm2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmLTTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46QTN2IN88UU4> MXvTRW5ITVJ?
human SW1710 cell MonwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWm3OWdmUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjR{NEW2JO69VS5? NWHibWUxW0GQR1XS

... 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=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