Novel, selective GRK2/3 inhibitor Cmpd101 launched by Hello Bio

June 15, 2015 - 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 uM 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 u-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