Drug intelligence / Profile preview

pyrazolanthrone

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
01

Overview

Pyrazolanthrone (SP600125) is a synthetic small molecule that acts as a potent, selective, and reversible inhibitor of c-Jun N-terminal kinases (JNKs), specifically targeting JNK1, JNK2, and JNK3 with nanomolar potency. It competitively inhibits ATP binding to these kinases and is over 300-fold more selective for JNKs compared to other MAP kinases such as ERK1 and p38. By inhibiting the phosphorylation of c-Jun, pyrazolanthrone suppresses the expression of inflammatory genes including COX‑2, IFN‑γ, IL‑2, TNF‑α and can block activation/differentiation in primary human CD4 cell cultures. It has also been shown to prevent apoptosis in various cell types and inhibit autophagy in HeLa cells. Pyrazolanthrone is primarily used as an experimental tool compound in research settings; it has not been approved for clinical use or marketed for any indication[1][5][9].

Other names
1,9-PyrazoloanthroneAnthra(1,9-cd)pyrazol-6(2H)-onePyrazoleanthroneDibenzo[cd,g]indazol-6(2H)-oneJNK Inhibitor II
02

Targets

JNK (Mitogen-activated protein kinase kinase kinase family)

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