TPCA-1

SKU: orb1224892

Description

A potent, selective and orally bioavailable IKK-2 inhibitor with IC50 of 63 nM, TNF cell IC50 of 0.4 uM; displays >100-fold selectivity over IKK-1.

Key Properties

• CAS Number: 507475-17-4
• MW: 279.2901
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₀FN₃O₂S
• SMILES: O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N
• Target: IκB kinase (IKK)
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: 10-12 weeks old male DBA/1 OlaHsd mice. Dosage: 3, 10, or 20 mg/kg. Administration: i.p. , b. i. d, from days 1 to 47. Result: Reduced the severity and delays the onset of CIA. Attenuated ex vivo antigen-induced T cell proliferation in CIA. Animal model: Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×106). Dosage: 10 mg/kg. Administration: Intraperitoneally daily. Result: The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(ETPCA-1), 0.680(EZD1839), and 0.837(Eobserved), respectively.
• In Vitro:
  Cell Viability Assay Cell line: human peripheral blood monocytes stimulated with LPS. Concentration: 0-10 μM. Incubation time: ~24 hours. Result: TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes. Cell Viability Assay Cell line: HCC827 and H1975 cells. Concentration: 0-10 μM. Incubation time: 0.5-2 hours. Result: Suppressed proliferation of HCC827 and H1975 cells. Led to a G2-M cell-cycle arrest in HCC827 but not A549. Western blot analysis. Cell line: HEK-293T cell lines. Concentration: 0-2 μM (before IL-2 or IFN-α treatment). Incubation time: 0.5-2 hours. Result: Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IKK-2 Inhibitor IV

Quick Database Links

Gene Symbol

IκB kinase (IKK)