RGS Protein Inhibitor

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.

CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gα_o protein-protein interaction in vitro with an IC₅₀ of 17 nM.

CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gα_o interaction, with an IC₅₀ value of 1.9 μM.

CCG-63808 is a selective, reversible RGS4 inhibitor with an IC₅₀ of 10 μM for the Gα_o-RGS4 interaction. CCG-63808 enhances the contractile response of lymphatic smooth muscle and potentiates agonist-mediated thoracic duct contraction. CCG-63808 can be used in research related to neuropathic pain and hypertension.

Usenamine A is an orally active natural dibenzofuran compound with multiple biological activities such as anti-inflammatory and anticancer effects. Usenamine A inhibits the AKT/mTOR/STAT3/ID1 signaling axis and induces ubiquitin-proteasome degradation of ID1. Usenamine A targets the TNF-TNFR2 complex, inhibits RGS2, and interferes with Myosin-9/actin cytoskeleton remodeling. Usenamine A induces apoptosis, autophagy and ROS-mediated endoplasmic reticulum stress in cancer cells, inhibits cancer cell proliferation and invasion, and reduces the production of pro-inflammatory cytokines. Usenamine A alleviates arthritis-related symptoms. Usenamine A can be used in studies related to liver cancer, non-small cell lung cancer, rheumatoid arthritis and ankylosing spondylitis.

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-2046 is a RGS4 inhibitor with an IC₅₀ of 4.3 μM against RGS4-Gα_o interaction signal.

CCG-4986 is an RGS protein inhibitor. CCG-4986 inhibits protein activity by covalently modifying the Cys-132 site of RGS4. CCG-4986 can be used to study diseases related to dysregulated G protein-coupled receptor (GPCR) signaling, such as Parkinson's disease and opioid addiction.

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.