Today Hello Bio announced the launch of a novel, potent and selective G-protein coupled receptor kinase 2 and 3 (GRK2/3) inhibitor, Cmpd101.

GRKs are key regulators of GPCR dependent and independent signalling pathways and play a crucial role in GPCR desensitization – the deactivation of GPCR elicited signalling. Hypo/hyper activity of GRKs have been linked to many pathophysiologies.

A recent Molecular Pharmacology paper by Lowe et al shows Cmpd101 to be a potent and selective GRK2/GRK3 inhibitor (IC₅₀ values are 35, 290 nM and 125 μM at GRK2, GRK3 and GRK5 respectively). It is cell permeable and can be used to study the roles of GRK2/3 in GPCR desensitization and other functions.

“Our team are particularly excited by this new GRK inhibitor- until now there haven't been many commercially available tools to selectively modulate GRK2 and 3 - so the launch of Cmpd101 should really help researchers investigate this key kinase.” Steve Roome, co-founder and Managing Director of Hello Bio

Hello Bio is the first life science supplier to offer Cmpd101 and it joins the company’s fast- growing range of affordable tools, which include opioid receptor tools such as DAMGO, Naloxone and Endomorphin-1 as well as many signalling and receptor tools: PD 98059, Y-27632, D-AP5, NBQX disodium salt and more.

Reference

Lowe JD1, Sanderson HS1, Cooke AE1, Ostovar M2, Tsisanova E1, Withey SL1, Chavkin C3, Husbands SM2, Kelly E1, Henderson G1, Bailey CP4.(2015) Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization. Mol Pharmacol. 2015 May 26. pii: mol.115.098293. [Epub ahead of print]: PubMed ID 26013542

Further information

Agonists, antagonists, antibodies, fluorescent tools…but Hello Bio is more than a catalogue of life science tools. We are a team of researchers and scientists, who genuinely want to support and promote life science research. Everything we do has this at its heart – we strive to make our range as affordable as possible, we listen to what you want, and we contribute financially where we can, to travel awards, grants and bursaries.  Not forgetting - we insist on the best quality possible: for products, for service and for technical support.

Trusted and affordable results- whilst supporting science – what could be better?

For more information visit www.hellobio.com

 

“”