TPCA-1

SKU: orb1304589

Description

TPCA-1 is a potent and selective inhibitor of IKK-2 (IKKβ), exhibiting an IC50 of 17.9 nM with significant selectivity over IKK-1 and other kinases. This small molecule is widely used in research to study NF-κB signaling in inflammatory and oncological contexts, both in vitro and in vivo.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 507475-17-4
• MW: 279.29
• Purity: 99.29% (May vary between batches)
• Formula: C₁₂H₁₀FN₃O₂S
• SMILES: NC(=O)Nc1sc(cc1C(N)=O)-c1ccc(F)cc1
• Target: IκB/IKK,STAT,Apoptosis
• Solubility: H2O:Insoluble;Ethanol:2.8 mg/mL (10.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.58 mM);DMSO:1 mg/mL (3.58 mM)

Bioactivity

• Target IC50:
  IKKβ:17.9 nM
• 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).
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TPCA 1, TPCA1, TPCA-1, STAT, Apoptosis, IκB, IκB kinase, inhibit, Inhibitor, I kappa B kinase, GW 683965, GW683965, GW-683965, IkB/IKK, IkB, IKK, IKK2 Inhibitor IV, IKK2

Compound Identifiers

PubChem CID

9903786