RGS Protein Inhibitor

Artemisinin B is an orally active sesquiterpene natural product with anti-neuroinflammatory activity, which can be found in Artemisia annua Linn.. Artemisinin B suppresses the TLR4-MyD88-NF-κB signaling pathway by reducing the protein levels of TLR4 and MyD88, as well as inhibiting the mRNA expression of NF-κB p65. Artemisinin B reduces the expression of pro-inflammatory cytokines and attenuates synaptic loss, which can be used for the research of cognitive and behavioral impairments in Alzheimer's disease. Artemisinin B shows no cytotoxicity against human cardiomyocytes and exhibits very weak binding to hERG, suggesting its potential for cardioprotective property research.

Z55660043 is a Regulator of G protein signaling-14 (RGS14) inhibitor with an IC₅₀ of 2.3  μM. Z55660043 selectively and non-covalently inhibits RGS14 GTPase-accelerating protein (GAP) activity without measurable cytotoxicity. Z55660043 can be used for central nervous system and metabolic disorders research.

CCG-50014 (Standard) is the analytical standard of CCG-50014. This product is intended for research and analytical applications. CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.