PKA

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.

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

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.

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.

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.

H-89 dihydrochloride (5-Isoquinolinesulfonamide) is a potent inhibitor of protein kinase A (PKA; IC50: 0.14 μM, Ki: 48 nM).

Bilobetin ameliorates insulin resistance by PKA-mediated phosphorylation of PPARα in rats fed a high-fat diet.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1 2 3, p70S6K, PKA, and ROCKI II.

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.

HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.

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).

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

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

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective, ATP-competitive inhibitor of pan-Akt, with IC50 values of 5 nM, 18 nM, and 8 nM for Akt1, Akt2, and Akt3, respectively.

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.

ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM for GRK2, 0.38±0.06 μM for GRK5, and 3.9±1 μM for GRK1.

GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).

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.

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

H-9 dihydrochloride is a potent protein kinase (PKA) inhibitor.H-9 Dihydrochloride significantly reduces the excitatory response to 5-HT at low concentrations.H-9 Dihydrochloride affects pharyngeal activity.H-9 Dihydrochloride inhibits signaling and cell growth of EGF ( H-9 Dihydrochloride inhibits EGF (epidermal growth factor)-dependent signaling and cell growth in epithelial cell lines.

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.

PKG inhibitor peptide TFA (82801-73-8 free base) is an inhibitor of ATP-competitive cGMP-dependent protein kinase (PKG).

BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.

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

A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

Rp-cAMPS sodium is a phosphorothioate analog of cAMP, a protein kinase A inhibitor and a membrane-permeable cAMP antagonist that inhibits cAMP-dependent protein kinases by blocking cAMP-induced conformational transitions, and can be used in the study of cardiovascular diseases.

MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).

NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.

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.

H-8 hydrochloride is a reversible and ATP-competitive PKA inhibitor. It can be used to study metabolic diseases.

GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD (cGMP sodium salt) , also known as cGMP, is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin. GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD activates protein kinase G (PKG) and modulates ion channel conductance, with signaling affecting diverse processes including smooth muscle relaxation and proliferation, phototransduction, and energy homeostasis.

AT7867 is a potent ATP-competitive inhibitor of Akt1 2 3 and p70S6K PKA with IC50 values of 32 nM, 17 nM, 47 nM, 85 nM, and 20 nM, respectively, exhibiting little activity outside the AGC kinase family.

A-674563 2HCl is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

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).

2-Aminopurine is a double-stranded RNA-dependent protein kinase, protein kinase R (PKR) inhibitor.

Exisulind (CP248) induces apoptosis through the activation of protein kinase G (PKG). Exisulind exhibits antineoplastic activity in solid tumour and haematological cancer cell lines and is an inhibitor of tumour growth in rodent models of colon, prostate, bladder, mammary and lung cancer.

PKG drug G1 targets PKG Iα C42. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

HA-100 is an inhibitor of protein kinase

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively[1], and also inhibits PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM), and myosin light chain kinase (MLCK) (Ki=7.4 μM).

CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).

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.

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16 46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

PKI 14-22 amide, myristoylated Acetate inhibit cAMP-dependent protein kinase (PKA) and blocks hyperalgesia produced by spinal administration of 8-bromo-cAMP.