550368-41-7
Chemical Structure
PNRI-299
- CAS. Nr.: 550368-41-7
- Formula:C21H15N5O4
- Molecular Weight:401.37
IUPAC Name: N-benzyl-2-(3-cyanophenyl)-1,3,7-trioxo-2,3,7,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazine-5-carboxamide
InChIKey: UPQJVNPKWQFAKQ-UHFFFAOYSA-N
SMILES: O=C1N2N(C(C(NCC3=CC=CC=C3)=O)=CC(C2)=O)C(N1C4=CC(C#N)=CC=C4)=O
Biological Activity: PNRI-299 is a selective AP-1 transcription inhibitor with an IC50 of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model[1][2][3].
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PNRI-299 | PNRI-299 is a selective AP-1 transcription inhibitor with an IC50 of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model. | |||||||||||||||||||||
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References
- [1]. Nguyen C, et al. Chemogenomic identification of Ref-1/AP-1 as a therapeutic target for asthma. Proc Natl Acad Sci U S A. 2003 Feb 4;100(3):1169-73. [Content Brief]
- [2]. Souza DG, et al. NF-kappaB plays a major role during the systemic and local acute inflammatory response following intestinal reperfusion injury. Br J Pharmacol. 2005 May;145(2):246-54. [Content Brief]
- [3]. Sun Yang, et al. Apurinic/apyrimidinic endonuclease/redox effector factor-1(APE/Ref-1): a unique target for the prevention and treatment of human melanoma. Antioxid Redox Signal. 2009 Mar;11(3):639-50. [Content Brief]
