Chemical Probes

High quality chemical probes are highly valuable reagents to explore biology of their target proteins. The most useful chemical probes meet five criteria:

  1. The chemical probe is a potent inhibitor of its primary target, ideally with an in vitro potency in biochemical assays < 100 nM.

  2. The chemical probe demonstrates selectivity over other proteins, with at least a 30-fold window over closely related targets in the same protein family.

  3. The chemical probe shows activity in cellular assays at or below a concentration of 1 µM.

  4. A close analog of the chemical probe that lacks activity on the primary target is available as a negative control compound.

  5. The chemical probe is publicly available without restrictions on its use.

Dark Kinases

SGC-UNC has generated high quality chemical probes for several dark kinases.

SGC-AAK1-1 for adaptor protein 2-associated kinase (AAK1) and BMP-2 inducible kinase (BMP2K)

SGC-GAK-1 for cyclin G-associated Kinase (GAK)

SGC-CK2-1 for casein kinase 2 (CSNK2)

SGC-CLK-1 for Cdc2-like kinases 1, 2, and 4 (CLK1/CLK2/CLK4)

SGC-CAMKK2-1 for calcium/calmodulin-dependent protein kinase kinase 2 and 1 (CAMKK2/CAMKK1)

SGC-STK17B-1 for serine/threonine kinase 17B (STK17B)

We have also collaborated with SGC scientists in Frankfurt, Campinas, and Oxford to release chemical probes for several additional kinases.