CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.
G0507 is a pyrrolopyrimidinedione compound that serves as a potent inhibitor of Escherichia coli growth, effectively inducing the extracytoplasmic σE stress response. It acts as a valuable chemical probe, specifically designed to dissect lipoprotein trafficking in Gram-negative bacteria. Notably, G0507 demonstrates strong inhibitory activity against the LolCDE ABC Transporter.
DHQZ 36 is a potent retrograde trafficking inhibitor. It has potent anti-parasite activity. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages (EC50: 13.63 μM).
CESTRIN is a cellulose synthase trafficking probe that acts by inhibiting cellulose deposition and interferes with the trafficking of cellulose synthase complexes and their associated proteins KORRIGAN1 and POM2/CSI1.
D011-2120 is an agent of antiviral that acts by blocking microtubule polymerization, disrupting the Golgi complex and inhibiting viral trafficking to the plasma membrane during virus egress.
PPQ-581 is an anti-influenza agent. PPQ-581 interrupts the crucial RNP trafficking, resulting in influenza replication inhibition, preventing virus-induced cytopathic effects.
SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat
PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3 Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB c mice with a dose of 1 mg kg of 3,5-dimethyl PIT-1 per day.