Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
TPCA-1
Cat No.
CEI-1559
Description
TPCA-1 is a selective inhibitor of IκB kinase-2 with IC50 values of 17.9 nM and 0.4 μM for IKK-2 and-1, respectively.
Product Overview
TPCA-1 is a novel, potent, and selective inhibitor of human IKK-2.Demonstration that IκB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-κB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-α and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment of rheumatoid arthritis.
CAS No.
507475-17-4
Molecular Weight
279.29
Purity
0.98
Storage
Desiccate at-20°C
Targets
IKK-2
IC50
17.9 nM; 0.4 μM
Molecular Formula
C12H10FN3O2S
Chemical Name
2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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.
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.
Download
Download Datasheet