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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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.

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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 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFnjNWtKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> MlLEV2FPT0WU
human GCT cell NF\tVXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFH2cHFKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwOk44OiCwTT6= M4C4T3NCVkeHUh?=
human 769-P cell NF7SVnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3Xt[GlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFQvQTlibl2u NYHjZnJIW0GQR1XS
human LOXIMVI cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkLpTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> MknvV2FPT0WU
human D-336MG cell NInaeFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXzJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OFYvOiCwTT6= MXjTRW5ITVJ?
human S-117 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUfJcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= M4Cz[HNCVkeHUh?=
human D-247MG cell NWHjUGhMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGHzb5dKdmirYnn0bY9vKG:oIHj1cYFvKERvMkS3UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PDhwNUKgcm0v NWHYfnlqW0GQR1XS
human TYK-nu cell MkXNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHNTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4QSEQvF2u MYnTRW5ITVJ?
human A498 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlXjTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zJO69VS5? MYPTRW5ITVJ?
human HepG2 cells MoC2SpVv[3Srb36gZZN{[Xl? NFXWfnE{KGh? NFr6e|VKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> M1jJR|IzOjZzMEKz
human BCPAP cell MmfFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETYR2NKdmirYnn0bY9vKG:oIHj1cYFvKEKFUFHQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PyEQvF2u Mmn1V2FPT0WU
human KYSE-180 cell NWf1VWR2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkjtTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> NUC2c|ZDW0GQR1XS
human MIA-PaCa-2 cell M1XJbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXFZXpiUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OkDPxE1w NFu1So1USU6JRWK=
human HCC1395 cell NVu3d3hHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzF|OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc5KM7:TT6= NGTzfIRUSU6JRWK=
human RS4-11 cell M{LFeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{CxXWlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u M3njZXNCVkeHUh?=
human NCI-H2122 cell MkHCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvOjhizszNMi=> MVfTRW5ITVJ?
human SNU-423 cell Mn;2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXP0PJpMUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{LkWg{txONg>? NUXCUHNHW0GQR1XS
human SK-LMS-1 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkfyTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPjRizszNMi=> MkjVV2FPT0WU
human RPMI-7951 cell M2XYN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfaTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNzFOwG0v NHnaOWtUSU6JRWK=
human COLO-829 cell M2C2RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOEK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk44PjV2IN88UU4> M2fYZXNCVkeHUh?=
human SCC-9 cell M4HnSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkjJTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= Mk[4V2FPT0WU
human A704 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJGE4ODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVIh|ryPLh?= NWTrUVVqW0GQR1XS
human HOP-62 cell NEH4c5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYHacII5UW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjN4MEW0JO69VS5? MnjjV2FPT0WU
human HCC1569 cell NX7NUJd[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFzZUGJKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G1Olkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjR6M{C1JO69VS5? M3rUb3NCVkeHUh?=
human A172 cell NUXON2ZrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHT1Z5FKdmirYnn0bY9vKG:oIHj1cYFvKEFzN{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlc2PDl6IN88UU4> NGLROJZUSU6JRWK=
human MOLT-16 cell NXfUXnpMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFzTOmZKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh6NUW2JO69VS5? MXPTRW5ITVJ?
human TE-15 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PjOmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> MknIV2FPT0WU
human OE19 cell NWrWTW5iT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;zTIpbUW6qaXLpeIlwdiCxZjDoeY1idiCRRUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PjR3MTFOwG0v NVzPU2U{W0GQR1XS
human MHH-ES-1 cell M{nOUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xPDV2NTFOwG0v Ml7wV2FPT0WU
human NKM-1 cell NITIT25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1jRbGlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE{QTdzIN88UU4> MmfQV2FPT0WU
human RCC10RGB cell NWf4TIMxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXhN4N3UW6qaXLpeIlwdiCxZjDoeY1idiCUQ1OxNHJISiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMkm0O|kh|ryP NXi1S5k3W0GQR1XS
human BxPC-3 cell NHHqb25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mmf1TY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlcxOzlzIN88UU4> NHjBfHBUSU6JRWK=
human ALL-PO cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHPGS5BKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDN6NUig{txONg>? MX3TRW5ITVJ?
human SK-OV-3 cell M4DJU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlzLTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46QTN2IN88UU4> MW\TRW5ITVJ?
human SW1710 cell MnTSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEjmVoJKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? M4PFNnNCVkeHUh?=

... 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