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.

Size Price Stock Quantity  
USD 90 In stock
USD 170 In stock
USD 570 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • 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.

Purity & Quality Control

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] GSK-3α [1]
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 MlTvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY[4V25RUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC5zNjDuUU4> NHnsNoRUSU6JRWK=
human GCT cell NIjpUWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGdEXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNyNj63NkBvVS5? MVrTRW5ITVJ?
human 769-P cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmDtTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUW4OE46QSCwTT6= NGGybXpUSU6JRWK=
human LOXIMVI cell NYDBbG03T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHizXFhKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02QDhwM{Kgcm0v MXTTRW5ITVJ?
human D-336MG cell NFvsWIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OFYvOiCwTT6= MnLDV2FPT0WU
human S-117 cell NXvacGZMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUTJcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= MmDPV2FPT0WU
human D-247MG cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlHoTY5pcWKrdHnvckBw\iCqdX3hckBFNTJ2N13HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQ5NjV{IH7NMi=> NIXsVXZUSU6JRWK=
human TYK-nu cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFc6KM7:TT6= MXTTRW5ITVJ?
human A498 cell NHrZUYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYT6NotHUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{KM7:TT6= NGXscVZUSU6JRWK=
human HepG2 cells NVTnVVFKTnWwY4Tpc44h[XO|YYm= NWnKU3M1OyCq MnrZTY5pcWKrdHnvckBw\iCJU1uzMYJmfGFiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6lb4Lwc5JifGmxbjDv[kBcO0ifZ3z1Z49{\SCrboTvJIdtgWOxZ3XuJIFnfGW{IEOgbJJ{KGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7n M3vCTFIzOjZzMEKz
human BCPAP cell M3mxSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7pfG9KdmirYnn0bY9vKG:oIHj1cYFvKEKFUFHQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PyEQvF2u Mn7HV2FPT0WU
human KYSE-180 cell NWmxcG9kT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLaTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> NXTn[XdkW0GQR1XS
human MIA-PaCa-2 cell NVfse3Z{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnUW|VKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke2JO69VS5? MYXTRW5ITVJ?
human HCC1395 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3mTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44QCEQvF2u MXjTRW5ITVJ?
human RS4-11 cell MoXSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2O3XWlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u NIDUZlVUSU6JRWK=
human NCI-H2122 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLDT5UyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4JO69VS5? M4TFOXNCVkeHUh?=
human SNU-423 cell NVKzd4VrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXfJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4Phfg+9lCCLQ{WwQVIvPSEQvF2u NGe5WWVUSU6JRWK=
human SK-LMS-1 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43PCEQvF2u NIX2N5RUSU6JRWK=
human RPMI-7951 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvN{m1NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi55IN88UU4> MnThV2FPT0WU
human COLO-829 cell MlPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13aeWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24Nlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjd4NUSg{txONg>? M2\aSnNCVkeHUh?=
human SCC-9 cell NF;kXlRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnzhTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= NGnzRnRUSU6JRWK=
human A704 cell NWHhWGdmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmLoTY5pcWKrdHnvckBw\iCqdX3hckBCPzB2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6wPFEzKM7:TT6= M1f3SnNCVkeHUh?=
human HOP-62 cell MlqxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2fjWGlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{PjB3NDFOwG0v Mnn1V2FPT0WU
human HCC1569 cell NYXVW3lOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnzToFKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G1Olkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjR6M{C1JO69VS5? MXTTRW5ITVJ?
human A172 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWLkbIRIUW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{44PTR7ODFOwG0v NX7SeZBEW0GQR1XS
human MOLT-16 cell NGjOU3BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{PlTmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDh3NU[g{txONg>? NXrMRVdWW0GQR1XS
human TE-15 cell NWfYR4xsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUj4PIpZUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTV|NEOg{txONg>? Ml3KV2FPT0WU
human OE19 cell NFzOc3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlfZTY5pcWKrdHnvckBw\iCqdX3hckBQTTF7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OlQ2OSEQvF2u Mly3V2FPT0WU
human MHH-ES-1 cell NU\IVopPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mnv6TY5pcWKrdHnvckBw\iCqdX3hckBOUEhvRWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODR3NEWg{txONg>? MnPBV2FPT0WU
human NKM-1 cell M3vEeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\a[GlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE{QTdzIN88UU4> MXfTRW5ITVJ?
human RCC10RGB cell NYnUeodmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo\yTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO M3zvNnNCVkeHUh?=
human BxPC-3 cell NYH0NY5XT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVf3WYNiUW6qaXLpeIlwdiCxZjDoeY1idiCEeGDDMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjdyM{mxJO69VS5? NIPwWJlUSU6JRWK=
human ALL-PO cell M{HPN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fWfGlvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45Ozh3ODFOwG0v NYjIc2N[W0GQR1XS
human SK-OV-3 cell NFuxeJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHWzSYlKdmirYnn0bY9vKG:oIHj1cYFvKFONLV;WMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl7M{Sg{txONg>? NWf1cWhUW0GQR1XS
human SW1710 cell M3HVNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjYR|FsUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjR{NEW2JO69VS5? MXHTRW5ITVJ?

... 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 78 mg/mL warmed (167.61 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 3.5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

GSK-3 Signaling Pathway Map

GSK-3 Inhibitors with Unique Features

Related GSK-3 Products

Tags: buy CHIR-99021 (CT99021) | CHIR-99021 (CT99021) supplier | purchase CHIR-99021 (CT99021) | CHIR-99021 (CT99021) cost | CHIR-99021 (CT99021) manufacturer | order CHIR-99021 (CT99021) | CHIR-99021 (CT99021) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID