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TPCA-1

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Purity:99.29%

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COA HNMR HPLC

TPCA-1

Catalog No. T3049Cas No. 507475-17-4

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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Pack Size	Price	Availability
2 mg	$38	In Stock
5 mg	$61	In Stock
10 mg	$97	In Stock
25 mg	$175	In Stock
50 mg	$288	In Stock
100 mg	$446	In Stock

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Product Introduction

Bioactivity

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.
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)
Alias	GW683965, IKK2 Inhibitor IV, TPCA1

Chemical Properties

Molecular Weight	279.29
Formula	C12H10FN3O2S
Cas No.	507475-17-4

Storage & Solubility Information

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

Solution Preparation Table

Ethanol

	1mg	5mg	10mg	50mg
10 mM	0.3581 mL	1.7903 mL	3.5805 mL	17.9025 mL
20 mM	0.1790 mL	0.8951 mL	1.7903 mL	8.9513 mL
50 mM	0.0716 mL	0.3581 mL	0.7161 mL	3.5805 mL
100 mM	0.0358 mL	0.1790 mL	0.3581 mL	1.7903 mL

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