Protein Kinase A (PKA)

Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.

H 89 dihydrochloride is a cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase.

AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors.

A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).

NH125 is a selective eEF-2 kinase inhibitor.

8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator.

Dibutyryl-cAMP is a cell-permeable PKA activator by mimicing the action of endogenous cAMP.

Synaptamide is a potent mediator for neurogenic differentiation of NSCs acting through PKA/CREB activation.

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively).

Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.