| Identification | Back Directory | [Name]
TPCA-1 | [CAS]
507475-17-4 | [Synonyms]
TPCA-1
CS-991
GW683965
GW683965A
TPCA-1(TPCA 1)
TPCA-1 USP/EP/BP
TPCA-1
IKK-2 Inhibitor IV
IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem
5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide
2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
3-ThiophenecarboxaMide, 2-[(aMinocarbonyl)aMino]-5-(4-fluorophenyl)-
5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide TPCA-1 | [Molecular Formula]
C12H10FN3O2S | [MDL Number]
MFCD09037541 | [MOL File]
507475-17-4.mol | [Molecular Weight]
279.29 |
| Chemical Properties | Back Directory | [Melting point ]
>217°C (dec.) | [Boiling point ]
442.6±45.0 °C(Predicted) | [density ]
1.490 | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear | [form ]
powder | [pka]
13.12±0.50(Predicted) | [color ]
white to light brown | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
TPCA-1 (507475-17-4) selective inhibitor of IκB kinase 2 (IKK2) (IC50 = 17.9 nM).1 Inhibits production of pro-inflammatory cytokines in arthritis and other animal models of inflammation.1,2 Also attenuates NLRP3 inflammasome activation in THP-1 myeloid cells, and suppresses IL1β-induced proliferation, migration, and invasion of HeLa cells.3,4 Continuous exposure to TPCA-1 promotes expansion of hematopoietic stem/progenitor cells (HSPCs) via improved glycolysis and limited ROS production.5 | [Uses]
TPCA-1 is a direct dual inhibitor for both IKKβ (IKK-2) and STAT3. It inhibits STAT3 phosphorylation, DNA binding, and transactivation in vivo. Synergistic treatment of TPCA-1 with tyrosine kinase inhibitors (TKIs) can potentially be a more effective method for treating cancers. | [Definition]
ChEBI: 2-(carbamoylamino)-5-(4-fluorophenyl)-3-thiophenecarboxamide is a member of thiophenes and an aromatic amide. | [Biological Activity]
Potent, selective inhibitor of I κ B kinase-2 (IKK-2) (IC 50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF- κ B nuclear localisation. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory. | [Biochem/physiol Actions]
TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation. | [in vitro]
determination of the activity of tpca-1 against ten selected kinases, cox-1 and cox-2, showed the compound to be ~550-fold selective for ikk-2 versus ten of these enzymes. tpca-1 inhibits lipopolysaccharide-induced human monocyte production of tnf-α, il-6, and il-8 with an ic50 of 170 to 320 nm [1]. | [in vivo]
prophylactic administration of tpca-1 at 3, 10, or 20 mg/kg resulted in a dose dependent reduction in the severity of murine collagen-induced arthritis. the significantly reduced disease severity and delay of disease onset resulting from administration of tpca-1 at 10 mg/kg were comparable to the effects of the antirheumatic drug, etanercept [1]. | [storage]
Store at -20°C | [References]
Podolin et al. (2005), Attenuation of murine collagen-induced arthritis by a novel, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation; Pharmacol. Exp. Ther., 312 373
Wang et al. (2021), TPCA-1 negatively regulates inflammation mediated by NF-kB pathway in mouse chronic periodontitis model; Oral Microbiol., 36 192
Unterreiner et al. (2021), Pharmacological inhibition of IKKb dampens NLRP3 inflammasome activation after priming in the human myeloid cell line THP-1; Biophys. Res. Commun., 545 177
Tao et al. (2021), IL-1b promotes cervical cancer though activating NF-κB/CCL-2; J. Exp. Pathol., 14 426
Sun et al. (2021), Continuous NF-κB pathway inhibition promotes expansion of human phenotypical hematopoietic stem/progenitor cells through metabolism regulation; Cell Res., 399 112468 |
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