Drug intelligence / Profile preview

UK-5099

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Topical
01

Overview

UK-5099 is a small molecule research compound that acts as a potent and selective inhibitor of the mitochondrial pyruvate carrier (MPC). By blocking the transport of pyruvate into the mitochondria, UK-5099 prevents its entry into the tricarboxylic acid (TCA) cycle, thereby shifting cellular metabolism away from oxidative phosphorylation (OXPHOS). This metabolic reprogramming has significant implications in various biological contexts, including cancer cell survival, stem cell differentiation, and immune response. UK-5099 is widely utilized as a pharmacological tool to study the role of mitochondrial pyruvate metabolism in diseases such as non-small cell lung cancer (NSCLC) and pancreatic adenocarcinoma. Additionally, it has been investigated for its potential to mitigate radiation-induced intestinal toxicity and to promote hair growth through topical application. Although it also inhibits plasma membrane monocarboxylate transporters (MCTs), its potency for MPC is several orders of magnitude higher.

Other names
2-cyano-3-(1-phenylindol-3-yl)acrylate2-CPIYA
02

Targets

MPC2 (Mitochondrial pyruvate carrier 2)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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