TPCA-1

Catalog # Availability Size / Price Qty
2559/10
TPCA-1 | CAS No. 507475-17-4 | IkB Kinase Inhibitors
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Description: Potent, selective inhibitor of IKKβ

Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide

Purity: ≥97%

Product Details
Citations (8)
Reviews

Biological Activity

TPCA-1 is a potent, selective inhibitor of IκB kinase (IKK) β (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKKα and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF-κB nuclear localization. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.

Technical Data

M.Wt:
279.29
Formula:
C12H10FN3O2S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
507475-17-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. A highly conserved NF-kappaB-responsive enhancer is critical for thymic expression of Aire in mice.
    Haljasorg U, Bichele R, Saare M, Guha M, Maslovskaja J, Kond K, Remm A, Pihlap M, Tomson L, Kisand K, Laan M, Peterson P
    Eur J Immunol, 2015;45(12):3246-56.
  2. Early spatiotemporal-specific changes in intermediate signals are predictive of cytotoxic sensitivity to TNF? and co-treatments
    LH Loo, NM Bougen-Zhu, WC Tan
    Sci Rep, 2017;7(0):43541.
  3. NF-kappaB and STAT1 control CXCL1 and CXCL2 gene transcription.
    Burke S, Lu D, Sparer T, Masi T, Goff M, Karlstad M, Collier J
    Am J Physiol Endocrinol Metab, 2014;306(2):E131-49.
  4. Regulation of the CCL2 Gene in Pancreatic beta-Cells by IL-1beta and Glucocorticoids: Role of MKP-1.
    Burke S, Goff M, Updegraff B, Lu D, Brown P, Minkin S, Biggerstaff J, Zhao L, Karlstad M, Collier J
    PLoS ONE, 2012;7(10):e46986.
  5. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IκB kinase 2, TPCA-1 (2-[aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and
    Podolin et al.
    J.Pharmacol.Exp.Ther., 2005;312:373
  6. IK-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma.
    Birrell et al.
    Am.J.Respir.Crit.Care Med., 2005;172:962
  7. IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic.
    Birrell et al.
    Mol.Pharmacol., 2006;69:1791
  8. CAR T Cells Targeting MISIIR for the Treatment of Ovarian Cancer and Other Gynecologic Malignancies
    A Rodriguez-, P Sharma, M Poussin, AC Boesteanu, NG Minutolo, SB Gitto, DK Omran, MK Robinson, GP Adams, F Simpkins, DJ Powell
    Mol. Ther., 2019;0(0):.
  9. Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer
    J O'Connell, J Porter, B Kroeplien, T Norman, S Rapecki, R Davis, D McMillan, T Arakaki, A Burgin, D Fox Iii, T Ceska, F Lecomte, A Maloney, A Vugler, B Carrington, BP Cossins, T Bourne, A Lawson
    Nat Commun, 2019;10(1):5795.
  10. Distinct and overlapping functions of glutathione peroxidases 1 and 2 in limiting NF-kappaB-driven inflammation through redox-active mechanisms
    SC Koeberle, A Gollowitze, J Laoukili, O Kranenburg, O Werz, A Koeberle, AP Kipp
    Redox Biol, 2019;28(0):101388.

Product Datasheets

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Citations for TPCA-1

The citations listed below are publications that use Tocris products. Selected citations for TPCA-1 include:

8 Citations: Showing 1 - 8

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