For research use only.

Catalog No.S2824 Synonyms: GW683965

35 publications

TPCA-1 Chemical Structure

CAS No. 507475-17-4

TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.

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10mM (1mL in DMSO) USD 220 In stock
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Selleck's TPCA-1 has been cited by 35 publications

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Biological Activity

Description TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.
NF-κB [3]
STAT3 [3]
IKK2 [1]
(Cell-free assay)
17.9 nM
In vitro

In a time-resolved fluorescence resonance energy transfer assay, TPCA-1 inhibits human IKK-2 activity with an IC50 of 17.9 nM. In addition, TPCA-1 is demonstrated to be ATP-competitive. Besides, TPCA-1 exhibits IC50 values of 400 nM and 3600 nM against IKK-1 and JNK3, respectively. TPCA-1 inhibits the production of TNF-α, IL-6, and IL-8 in a concentration-dependent manner, exhibiting IC50 values of 170, 290, and 320 nM, respectively. [1] TPCA-1 inhibits glioma cell proliferation, as well as TNF-induced RelA (p65) nuclear translocation and NFκB-dependent IL8 gene expression. Importantly, TPCA-1 inhibits IFN-induced gene expression, completely suppressing MX1 and GBP1 gene expression, while having only a minor effect on ISG15 expression. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C57BL/6 mouse BMDM cells M{LFTWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYqyOEBp NIPzW5BEgXSxdH;4bYNqfHliYXfhbY5{fCCFNUfCUE83KG2xdYPlJGJOTE1iY3XscJMh[XO|ZYPz[YQh[XNiTFTIJJJmdGWjc3WgZYZ1\XJiMkSgbJJ{ MXWyNlU{Ozd7MB?=
C57BL/6 mouse BMDM cells NFW1V4JHfW6ldHnvckBie3OjeR?= M171clAvPSEQvF2= MYOxJIg> M17WRmFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hSzV5QlyvOkBud3W|ZTDCUWROKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNXO2aX31cIF1\WRiVF7GZYxxcGFicILv[JVkfGmxbjDheEAxNjVidV2gdJJmfHKnYYTl[EBnd3JiMTDodkBj\W[xcnWgUHBUKGOqYXzs[Y5o\SCjZoTldkA5KHSxIEK0JIhzeyCkeTDpcY12dm:jc4PhfS=> MkjKNlI2OzN5OUC=

... Click to View More Cell Line Experimental Data

In vivo

Prophylactic administration of TPCA-1 at 3, 10, or 20 mg/kg, i.p., b.i.d., results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA). The significantly reduced disease severity and delay of disease onset resulting from administration of TPCA-1 at 10 mg/kg, i.p., b.i.d. are comparable to the effects of the antirheumatic drug, etanercept, when administered prophylactically at 4 mg/kg, i.p., every other day. Nuclear localization of p65, as well as levels of IL-1beta, IL-6, TNF-alpha, and interferon-gamma, is significantly reduced in the paw tissue of TPCA-1- and etanercept-treated mice. In addition, administration of TPCA-1 in vivo results in significantly decreased collagen-induced T cell proliferation ex vivo. Therapeutic administration of TPCA-1 at 20 mg/kg, but not at 3 or 10 mg/kg, i.p., b.i.d., significantly reduces the severity of CIA, as does etanercept administration at 12.5 mg/kg, i.p., every other day. [1]


Kinase Assay:


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IKK-2 Assay:

Recombinant human IKK-2 (residues 1-756) is expressed in baculovirus as an N-terminal GST-tagged fusion protein, and its activity is assessed using a time-resolved fluorescence resonance energy transfer assay. In brief, IKK-2 (5 nM final) diluted in assay buffer (50 mM HEPES, 10 mM MgCl2, 1 mM CHAPS, pH 7.4, with 1 mM DTT and 0.01% w/v BSA) is added to wells containing various concentrations of compound or dimethyl sulfoxide (DMSO) vehicle (3% final). The reaction is initiated by the addition of GST-IκBα substrate (25 nM final)/ATP (1 μM final), in a total volume of 30 μL. The reaction is incubated for 30 min at room temperature, then terminated by the addition of 15 μL of 50 mM EDTA. Detection reagent (15 μL) in buffer (100 mM HEPES, pH 7.4, 150 mM NaCl, and 0.1% w/v BSA) containing antiphosphoserine- IκBα-32/36 monoclonal antibody 12C2, labeled with W-1024 europium chelate, and an allophycocyanin-labeled anti-GST antibody is added, and the reaction is further incubated for 60 min at room temperature. The degree of phosphorylation of GST- IκBαis measured as a ratio of specific 665-nm energy transfer signal to reference europium 620-nm signal, using a Packard Discovery plate reader.
Cell Research:


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  • Cell lines: U87, MT330, SJ-G2, and GBM6 human glioma lines
  • Concentrations: 0-50 μM
  • Incubation Time: 3 days
  • Method:

    Ten microliters of 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) from stock solution (10 mg/mL) is added to each well of 96-well plates containing glioma cells and incubated at 37 °C for 2–4 h. Oxidized MTT is solubilized by adding 100 μL of 10% sodium dodecyl sulfate (SDS) in 0.01 N HCL, and plates are incubated at 37 °C for 4 h in a humidified chamber. Plates are read at 570 nm on a plate reader.

    (Only for Reference)
Animal Research:


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  • Animal Models: Murine collagen-induced arthritis
  • Dosages: 3, 10, or 20 mg/kg
  • Administration: Administered via i.p. or b.i.d.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (200.5 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% Cremophor EL, 2% N,N-dimethylacetamide
For best results, use promptly after mixing.
15 mg/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 279.29


CAS No. 507475-17-4
Storage powder
in solvent
Synonyms GW683965
Smiles C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID