NF-κB Agonist

Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC₅₀=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC₅₀=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.

Berubicin (RTA 744) hydrochloride is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin hydrochloride inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin hydrochloride exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin hydrochloride can be used in the study of tumors related to the nervous system.

ULK1-IN-3 (Compound 8) is a novel chromone-based as a potential inhibitor of ULK1. ULK1-IN-3 inhibits cell cycle, autophagy and induces apoptosis, oxidative stress in colon cancer cell lines.

PapRIV is an agonist of BV-2 microglial cells, capable of activating microglial cells through an NF-κB-dependent pathway. PapRIV induces the expression of pro-inflammatory cytokines such as IL-6 and TNFα and increases the production of reactive oxygen species (ROS). PapRIV can cross the blood-brain barrier.

Anti-inflammatory agent 88 (compound 6) is a carbazole derivative with anti-inflammatory activity found in marine Streptomyces. It exerts its anti-inflammatory effect by inhibiting pro-inflammatory factors and enhancing the expression of anti-inflammatory factors in the Myd88/Nf-κB pathway. Anti-inflammatory agent 88 can be used for the development of anti-inflammatory drugs.

TLR2 agonist 1 (Compound R-7d) is an agonist for human toll-like receptor 2 (TLR 2) with an EC₅₀ of 116 pM. TLR2 agonist 1 enhances NF-κB promoter activation through TLR2/TLR1 heterodimers.