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 307 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 NH2wW5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XEbGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvOTZibl2u MWXTRW5ITVJ?
human GCT cell NF;2WWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2ewN2lvcGmkaYTpc44hd2ZiaIXtZY4hT0OWIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{C2MlczKG6PLh?= M1HZOXNCVkeHUh?=
human 769-P cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYXJcohq[mm2aX;uJI9nKGi3bXHuJFc3QS2SIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUi0Mlk6KG6PLh?= NIjEcHRUSU6JRWK=
human LOXIMVI cell M2f6NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXj1UmRHUW6qaXLpeIlwdiCxZjDoeY1idiCOT2jJUXZKKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PTh6LkOyJI5ONg>? Ml\PV2FPT0WU
human D-336MG cell Mn;NS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{W4d2lvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg1Pi5{IH7NMi=> NGqzcJNUSU6JRWK=
human S-117 cell NIDzTZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVryRphiUW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> MV3TRW5ITVJ?
human D-247MG cell NIeybWhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGQuOjR5TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OFgvPTJibl2u MlroV2FPT0WU
human TYK-nu cell M33KWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlrQTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u Mn;kV2FPT0WU
human A498 cell NYPaOIV7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rrU2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR7ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN{DPxE1w NY\HOYF2W0GQR1XS
human HepG2 cells MkPJSpVv[3Srb36gZZN{[Xl? NULncXh2OyCq NEnXTnpKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> M2ro[|IzOjZzMEKz
human BCPAP cell NUDESIM6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w NGnVbo9USU6JRWK=
human KYSE-180 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NILEWIJKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55MzFOwG0v NF;ie|dUSU6JRWK=
human MIA-PaCa-2 cell Mmj6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd4IN88UU4> MYPTRW5ITVJ?
human HCC1395 cell NX\UVZRRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXTIbWQ{UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxN|k2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55ODFOwG0v NV3Z[llxW0GQR1XS
human RS4-11 cell MoDQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnjCTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2KM7:TT6= NV\KV|duW0GQR1XS
human NCI-H2122 cell NG\acotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEjNRpJKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlEzOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMkig{txONg>? MlzMV2FPT0WU
human SNU-423 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4Phfg+9lCCLQ{WwQVIvPSEQvF2u NFLCUVBUSU6JRWK=
human SK-LMS-1 cell MnfzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH75[5VKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi54NDFOwG0v MnjrV2FPT0WU
human RPMI-7951 cell MlTZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH36dFBKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? M3Xle3NCVkeHUh?=
human COLO-829 cell MljWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4K2V2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24Nlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjd4NUSg{txONg>? MXvTRW5ITVJ?
human SCC-9 cell NXj1epN5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\Hb3dmUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTVizszNMi=> NFjjVotUSU6JRWK=
human A704 cell NVjWU2NvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXiwW5hIUW6qaXLpeIlwdiCxZjDoeY1idiCDN{C0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4xQDF{IN88UU4> NGfI[I1USU6JRWK=
human HOP-62 cell NUHEV5RNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;QTY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlM3ODV2IN88UU4> NWqwPJJWW0GQR1XS
human HCC1569 cell NEnGUnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXP6T2l1UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxOVY6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy52OEOwOUDPxE1w M2TJZ3NCVkeHUh?=
human A172 cell NVmwS2FlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NILpZVRKdmirYnn0bY9vKG:oIHj1cYFvKEFzN{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlc2PDl6IN88UU4> MY\TRW5ITVJ?
human MOLT-16 cell NYH2OYJ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFqydo9KdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh6NUW2JO69VS5? MlzqV2FPT0WU
human TE-15 cell M2X2Rmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHTmNYxKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PTN2MzFOwG0v MlS1V2FPT0WU
human OE19 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LYOmlvcGmkaYTpc44hd2ZiaIXtZY4hV0VzOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVY1PTFizszNMi=> MYPTRW5ITVJ?
human MHH-ES-1 cell MnTTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2PROWlvcGmkaYTpc44hd2ZiaIXtZY4hVUiKLVXTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB2NUS1JO69VS5? NYfDNXBlW0GQR1XS
human NKM-1 cell NI\ibVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFztRW9KdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v MoGxV2FPT0WU
human RCC10RGB cell NYqw[nNpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGr0XoZKdmirYnn0bY9vKG:oIHj1cYFvKFKFQ{GwVmdDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5{OUS3PUDPxE1? NXPObIZCW0GQR1XS
human BxPC-3 cell MoTkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXTjcYs6UW6qaXLpeIlwdiCxZjDoeY1idiCEeGDDMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjdyM{mxJO69VS5? NWfYO|dyW0GQR1XS
human ALL-PO cell Mn7ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFM5PThizszNMi=> M{XOdXNCVkeHUh?=
human SK-OV-3 cell M2jJcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NELPdWJKdmirYnn0bY9vKG:oIHj1cYFvKFONLV;WMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl7M{Sg{txONg>? MX\TRW5ITVJ?
human SW1710 cell MlHES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGHGfGlKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? MXzTRW5ITVJ?

... 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

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID