A selective inhibitor of IKK2 (IC50s = 17.9 nM and 0.40 μM for IKK2 and IKK1

TPCA-1 – 500 µg

Brand:
Cayman
CAS:
507475-17-4
Storage:
-20
UN-No:
Non-Hazardous - /

TPCA-1 is a selective inhibitor of IκB kinase-2 (IC50s = 17.9 nM and 0.40 μM for IKK2 and IKK1, respectively).{24239} Furthermore, it displays greater than 550-fold selectivity over other kinases and enzymes including, p38, MAPK, COX, and JNK.{24239} TPCA-1 inhibits the production of LPS-induced TNF-α, IL-6, and IL-8 with IC50 values equal to 0.17, 0.29, and 0.32 μM, respectively.{24239} At 20 mg/kg, TPCA-1 has been used to reduce the severity and onset of collagen-induced arthritis in mice and at 30 mg/kg to block cytokine release in an antigen-driven rat model of lung inflammation.{24239,24240}  

 

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Description

A selective inhibitor of IKK2 (IC50s = 17.9 nM and 0.40 μM for IKK2 and IKK1, respectively); reduces the severity and onset of collagen-induced arthritis in mice and blocks cytokine release in an antigen-driven rat model of lung inflammation

Formal name: 2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide

Synonyms:  IKK2 Inhibitor IV

Molecular weight: 279.3

CAS: 507475-17-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|IKKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition||Research Area|Immunology & Inflammation|Innate Immunity|STING||Research Area|Infectious Disease

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