Drug intelligence / Profile preview

SC-514

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

SC-514 is a potent, selective, and reversible small molecule inhibitor of IκB kinase-2 (IKK-2, also known as IKKβ). It functions by competing with ATP for the binding site on the IKK-2 enzyme, which prevents the phosphorylation and subsequent degradation of IκBα. This inhibition blocks the nuclear translocation of the transcription factor NF-κB, thereby suppressing the expression of NF-κB-dependent genes involved in inflammation and cell survival, such as BCL2. SC-514 is widely utilized as a pharmacological research tool to study the NF-κB signaling pathway in various disease contexts, including oncology and inflammatory disorders. Preclinical studies have demonstrated its ability to induce apoptosis in tumor cells and delay tumor growth in vivo, often by sensitizing cells to other metabolic or energetic stressors.

Other names
4-Amino-[2,3'-bithiophene]-5-carboxamideGK-01140GK01140GK 01140
02

Targets

IKBKB (IKKβ)

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