PKA

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.

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.

PKG Substrate acetate is a selective substrate for cGMP-dependent protein kinase (PKG).PKG Substrate is a selective substrate for protein kinase G (PKG) with a strong preference for PKG Iα (Km = 59 μM) over PKG II (Km = 305 μM).

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

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.

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.

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

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

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

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).

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

PKI (5-24) Acetate is a high affinity PKA inhibitor (Ki = 2.3 nM).

AP-C2 is a potent small molecule guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) inhibitor with a pIC50 of 5.2 for cGKII.

HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein

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).

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.

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

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.

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

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively).

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).

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.

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.

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.

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.

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

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

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

Ellagic acid (Gallogen) is a fused four ring compound isolated from the kino of Eucalyptus maculata Hook and E. Hemipholia F. Muell. Activates Factor XII of the blood clotting system which also causes kinin release; used in research and as a dye.

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.

HA-100 is an inhibitor of protein kinase

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.

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.

PKItide demonstrates an inhibitory concentration 50 (IC50) of 0.2 μM against cAMP-dependent protein kinase (cAMP-PK) [1].

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

Protein kinase G inhibitor-1 is a potent Protein kinase G inhibitor, IC50= 0.9 uM.

Warangalone is an anti-malarial compound that can inhibit the growth of both strains of parasite 3D7 (chloroquine-sensitive) and K1 (chloroquine-resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively.

Cycloheterophyllin has an antioxidant effect, it is a photoprotective agent that inhibits ultraviolet A (UVA)-induced oxidative stress and damage, and could be used in the research on and prevention of skin photoaging.

alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats. alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki=6 microM), it also shows weak cytotoxicity against the A2780 human ovarian cancer cell line.

Aplithianines A effectively inhibits J-PKAcα with an IC50 value of 1 μM and displays higher potency against wild-type PKA, achieving an IC50 of 84 nM by competitively interacting with the ATP pocket [1].

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.

Isopedicin has anti-inflammatory functions, it inhibits the O(2)(*)(-) production in human neutrophils by an elevation of cellular cAMP and activation of PKA through its inhibition of cAMP-specific PDE.

Gliotoxin, a Wnt signaling pathway inhibitor, induces growth inhibition and apoptosis in multiple colorectal cancer cell lines with mutations of the Wnt signaling pathway.

Kemptide is a synthetic heptapeptide, acting as a substrate for cAMP-dependent protein kinase (PK).

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

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

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.

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.