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TPCA-1

Catalog No. T3049 CAS 507475-17-4

Synonyms: GW683965, IKK2 Inhibitor IV, TPCA1

TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows <22-fold selectivity over IKK-1 and <550-fold selectivity over others kinases and enzymes.

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TPCA-1, CAS 507475-17-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 175.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 446.00

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Purity: 99.29%

Purity: 95.03%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes.
Targets&IC50	IKK2:17.9 nM
In vitro	TPCA-1 significantly reduces collagen-induced T-cell proliferation in vivo. Administering TPCA-1 (3/10/20 mg/kg, i.p., b.i.d.) prophylactically results in a dose-dependent reduction in the severity of collagen-induced arthritis (CIA) in mice. Specifically, TPCA-1 at 20 mg/kg (i.p., b.i.d.) markedly decreases the severity of CIA, an effect comparable to that of etanercept (12.5 mg/kg, i.p.) administered every other day. Additionally, TPCA-1 at 10 mg/kg (i.p., b.i.d.) significantly diminishes disease severity and delays disease onset, mirroring the efficacy of etanercept (4 mg/kg, i.p.) given every other day as a preventive measure.
In vivo	TPCA-1 exhibits concentration-dependent inhibition of TNF-α (IC50: 170 nM), IL-6 (IC50: 290 nM), and IL-8 (IC50: 320 nM) production. It also suppresses the proliferation of glioma cells, TNF-induced nuclear translocation of RelA (p65), and NFκB-dependent IL8 gene expression. Furthermore, TPCA-1 inhibits gene expression induced by IFN, completely blocks the expression of the MX1 and GBP1 genes, and has a minimal effect on ISG15 expression. Additionally, TPCA-1 demonstrates inhibition of IKK-1 (IC50: 400 nM) and JNK3 (IC50: 3600 nM).
Kinase Assay	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	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)

Synonyms	GW683965, IKK2 Inhibitor IV, TPCA1
Molecular Weight	279.29
Formula	C12H10FN3O2S
CAS No.	507475-17-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

Ethanol: 2.8 mg/mL (10 mM)

DMSO: 1 mg/mL, Sonification is recommended.

References and Literature

1. Podolin PL, et al, J Pharmacol Exp Ther, 2005, 312(1), 373-381. 2. Du Z, et al, J Interferon Cytokine Res, 2012, 32(8), 368-377. 3. Luebke T, Schwarz L, Beer Y Y, et al. c-FLIP and CD95 signaling are essential for survival of renal cell carcinoma[J]. Cell death & disease. 2019 May 16;10(6):384.

Citations

1. Luebke T, Schwarz L, Beer Y Y, et al. c-FLIP and CD95 signaling are essential for survival of renal cell carcinoma. Cell Death & Disease. 2019 May 16;10(6):384

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library NF-κB Signaling Compound Library Anti-Pancreatic Cancer Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Anti-Ovarian Cancer Compound Library Anti-Cancer Metabolism Compound Library Pyroptosis Compound Library HIF-1 Signaling Pathway Compound Library JAK-STAT Compound Library

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Keywords

TPCA-1 507475-17-4 Apoptosis JAK/STAT signaling NF-Κb Stem Cells STAT IκB/IKK GW 683965 Inhibitor TPCA 1 IKK I kappa B kinase GW-683965 GW683965 IKK2 Inhibitor IV IκB kinase TPCA1 inhibit inhibitor

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