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CHIR-99021 (CT99021)

Catalog No.S1263 1 Review(s)
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CHIR-99021 (CT99021) Chemical Structure

  • SB 216763

    SB 216763 inhibited human GSK-3α with IC50s of 34 nM.

  • TWS119

    TWS119 is a glycogen synthase kinase-3β inhibitor with an IC50 of 30 nM.

  • Indirubin

    Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 75 nM and 0.19 μM.

  • SB 415286

    SB 415286 is a potent and selective cell-permeable, ATP-competitive GSK3α inhibitor with an IC50 and a Ki of 78 and 31 nM, respectively.

  • CHIR-98014

    CHIR 98014 is a potent and selective human GSK-3 inhibitor for human GSK-3ɑ and human GSK-3β with IC50 of 0.65 nM and 0.58 nM, respectively.

  • BEZ235 (NVP-BEZ235)

    BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.

  • Deforolimus (Ridaforolimus)

    Deforolimus (Ridaforolimus) is a small-molecule inhibitor of mTOR.

  • Perifosine

    Perifosine is an Akt inhibitor. the antiproliferative properties of perifosine with an IC50 of 0.6–8.9 µM.

  • PI-103

    PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.

  • Rapamycin (Sirolimus)

    Rapamycin also known as Sirolimus & Rapamune is an mTOR inhibitor. Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated pathways.

Biological Activity

CHIR-99021 (CT99021) is a glycogen synthase kinase 3β (GSK3β) inhibitor that has antiproliferative activity in vitro and in vivo. [1] CHIR-99021 inhibits GSK-3 with IC50 at 7 nM. In a series of carcinoma cell lines, the IC50 of CHIR99021 for proliferation is about 10μM. [1] CHIR-99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) with 350-fold selectivity toward GSK-3β compared to CDKs . [1]

References on CHIR-99021 (CT99021)
  • [1] BMC Cell Biology 2007;8:34
Molecular Weight (WM): 465.34
Formula:

C22H18Cl2N8

CAS No.: 252917-06-9
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥3mg/mL 
Water <1mg/mL 
Ethanol <1mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

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COA H-NMR HPLC

Research Area

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Related Inhibitors

Recommended Screening Libraries

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    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. 

  • 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. 

  • Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.
    CHIR-99021 (CT99021) purchased from Selleck

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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. 

Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.

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