PKA

PKA inhibitor fragment (6-22) amide Acetate is a synthetic peptide which selectively inhibits PKA activity by binding to its substrate site (IC50 < 2 nM).

PKA-IN-1 is a selective and potent cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor (IC50: 0.03 μM).PKA-IN-1 can be used to study diseases of the immune system.

PKA Inhibitor Fragment (6-22) amide TFA (PKA Inhibitor Fragment (6-22) amide TFA) is a highly potent inhibitor of cAMP-dependent protein kinase A (PKA) with a Ki of 2.8 nM and reverses the pain-relieving effects of low levels of morphine in mice.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt) is a long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase（PKA）, but resistant to degradation by cyclic AMP phosphodiesterase.

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

LX-7101 hydrochloride is a potent LIMK and ROCK2 inhibitor with antihypertensive activity, inhibits LIMK1/2, ROCK, PKA, and can be used to study glaucoma.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Metadoxine (Metadoxil) is a neurotransmitter stimulant.

Malantide acetate is a dodecapeptide phosphorylated by cyclic AMP-dependent protein kinase (PKA), and increases PKA activity.Malantide is a synthetic peptide that is phosphorylated by PKA and is used to measure PKA activity in vitro.

CREBtide acetate is a synthetic substrate for PKA (Km=3.9 μM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).

H-89 is a selective and potent protein kinase A inhibitor (IC50: 48 nM), a candidate cardioprotectant, induces spatial learning impairment in rats, and can be used to study myocardial infarction.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

K-252a is a protein kinase inhibitor targeting serine-threonine, tyrosine, and CAM kinases. In vitro, it blocks NGF-induced TrkA signalling and neural differentiation, exhibiting antitumour, antibacterial, anti-inflammatory, and neuroprotective activities.

KT5720 is a cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase A (PKA) (Ki: 60 nM).

KT5823 is a selective and potent cGMP-dependent protein kinase (PKG) inhibitor with inhibitory effects on PKA and PKC.KT5823 increases thyroid-stimulating hormone-induced (Na+/I- symporter) NIS expression and iodide ion uptake by modulating sodium iodide symporter protein expression and activity in thyroid cells. KT5823 induces apoptosis.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.