Activators & Inhibitors

CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator (EC 50= 100 nM). CXCR4 modulator-1 has research value in anti-inflammatory, anticancer and anti-HIV.

Mazaticol is an anticholinergic agent, which blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol potently inhibits 3H-QNB and 3H-PZ binding. Mazaticol can bind to the M2 receptors with high affinity. Mazaticol shows inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol has research in parkinsonian syndrome.

EGFR-IN-71 is a potent inhibitor of epidermal growth factor receptor (EGFR) (IC50= 3.7 μM). EGFR-IN-71 has research value in chordoma.

HIV-1 inhibitor-20 is a potent HIV-1 inhibitor.

LDN-209929 dihydrochloride is a potent and selective inhibitor of haspin kinase (IC50= 55 nM). LDN-209929 dihydrochloride shows180-fold selectivity verses DYRK2 (IC50= 9.9 μM).

Antiproliferative agent-8 (Compound 5a) is an anti-cancer compoundwith antiproliferative activity. Antiproliferative agent-8 can significantly increase the P53 levels.

PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50= 2 nM). In hepatocellular carcinoma models, PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis.

(R,R)-BAY-Y 3118, the R-enantiomer of BAY-Y 3118, exhibits weak bactericidal activity.

PqsR/LasR-IN-1 (Compound 2a) is a potent inhibitor of LasR and PqsR systems in P. aeruginosa. PqsR/LasR-IN-1 is also a inhibitor of hERG (IC50= 6.77 μM).