Catalog No.S2824 Synonyms: GW683965
Molecular Weight(MW): 279.29
TPCA-1 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.
Cited by 8 Publications
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GAB2-induced chemokine expression is dependent on IKKβ-NF-κB activity. (a) Effect of small-molecule inhibitors against PI3K (GDC-0941), PI3K/mTOR (BEZ235), MEK (AZD6288) or IKKβ (TPCA-1, IKK16 and Bay 65–1942) on CXCL1, CXCL2 and CXCL8 mRNA levels in GAB2-overexpressing FTSECs. Cells were treated with 2 μm of each inhibitor or DMSO control for 6 h before collected for quantitative PCR analyses. Data are averages±s.e.m. of four independent experiments. Comparison between DMSO- or inhibitor-treated GAB2-overexpressing FTSECs were used for statistical analyses. n.s., not significant; *P<0.05; **P<0.01. (b) Effect of suppressing IKKβ (encoded by IKBKB) or NF-κB p65 (encoded by RELA) on CXCL1, CXCL2 and CXCL8 mRNA levels in GAB2-overexpressing FTSECs. Cells were infected with a control shRNA targeting LacZ or shRNAs targeting IKBKB or RELA and cultured for 48 h before collected for quantitative PCR analyses. Data are averages±s.e.m. of three independent experiments. *P<0.05; **P<0.01.
Oncogene, 2016, 35(31):4036-47. TPCA-1 purchased from Selleck.
(D and E) quantitative real-time PCR for the transcript expression levels of NLRP3 and IL-1b in NP cells induced by AGEs-BSA for 48 hrs, single or combined with RAGE-Ab or TPCA-1. Data were presented as mean ± S.D. (n = 3). *P < 0.05 versus control, #P < 0.05 versus AGEs-BSA.
J Cell Mol Med, 2017. TPCA-1 purchased from Selleck.
AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
Mol Cancer 2014 13, 40. TPCA-1 purchased from Selleck.
Requirement of IKK activation for insulin-dependent induction of IL-1 in U937 macrophages. U937 cells were pretreated with 1 μM PD-98059 or 5 μM 2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide (TPCA-1) for 90 min and subsequently stimulated with 100 nM insulin for 24 h. IL-1 mRNA was quantified as detailed in the legend to Fig. 1. Values are means ± SE of the no. of experiments indicated. Statistics: Student's t-test for unpaired samples and (where appropriate) 2-way ANOVA with Tukey's test for multiple comparison. *P < 0.05.
Am J Physiol Endocrinol Metab, 2016, 310(11):E938-46. TPCA-1 purchased from Selleck.
Honokiol regulated the expression of PTX3 and inflammatory response in PA-induced HUVECs model. PTX-3 levels from the enzyme-linked immunosorbent assay (ELISA) in HUVECs after treatment with vehicle, 0.5 mM PA, PA plus 10 μM honokiol or PA plus an inhibitor of IKK-2 (TPCA-1, 30 μM) for 48 h.
Exp Mol Med, 2015, 10.1038/emm.2015.37. TPCA-1 purchased from Selleck.
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|Description||TPCA-1 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.|
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.  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. 
|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. |
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.
|In vitro||DMSO||56 mg/mL (200.5 mM)|
|Water||slightly soluble or insoluble|
|Ethanol||slightly soluble or insoluble|
|In vivo||2% Cremophor EL, 2% N,N-dimethylacetamide||15 mg/mL|
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