1. Signaling Pathways
  2. Stem Cell/Wnt
    TGF-beta/Smad
  3. PKA

PKA

Protein kinase A

PKA (Protein kinase A) is a Ser/Thr phosphoryl transferase that transfers the γ-phosphate group of ATP to protein substrates. PKA phosphorylates more than 100 cytoplasmic and membrane associated targets. PKA mediates a myriad of cellular signaling events and its activity is tightly regulated both in space and time.

PKA is an evolutionarily conserved negative regulator of the hedgehog (Hh) signal transduction pathway. PKA is known to be required for the proteolytic processing event that generates the repressor forms of the Ci and Gli transcription factors that keep target genes off in the absence of Hh.

PKA Isoform Specific Products:

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N6727
    Gliotoxin
    Activator 99.51%
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells. Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells.
    Gliotoxin
  • HY-N6789
    KT5720
    Inhibitor ≥99.0%
    KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases.
    KT5720
  • HY-16071
    AT13148
    Inhibitor 99.21%
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
    AT13148
  • HY-B1899
    Taurodeoxycholic acid
    Activator ≥98.0%
    Taurodeoxycholate sodium salt is a bile salt-related anionic detergent. Taurodeoxycholic acid is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholic acid is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholic acid (TDCA) exhibits anti-inflammatory and neuroprotective effects.
    Taurodeoxycholic acid
  • HY-12059
    AT7867
    Inhibitor 99.88%
    AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
    AT7867
  • HY-P1290A
    PKA Inhibitor Fragment (6-22) amide TFA
    Inhibitor 99.87%
    PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice.
    PKA Inhibitor Fragment (6-22) amide TFA
  • HY-107574
    TC-E 5003
    Activator 98.03%
    TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.
    TC-E 5003
  • HY-P4860
    Adropin (34-76) (human, mouse, rat)
    Inhibitor 99.92%
    Adropin (34-76) is a secretory domain of Adropin. Adropin (34-76) can inhibit cAMP level and glucose production in hepatocytes, and has a hypoglycemic effect. Adropin (34-76) plays an antifibrotic role by inhibiting the GLI1 signaling pathway.
    Adropin (34-76) (human, mouse, rat)
  • HY-P1291
    PKI 14-22 amide,myristoylated
    Inhibitor 99.65%
    PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
    PKI 14-22 amide,myristoylated
  • HY-P0222
    PKI(5-24)
    Inhibitor 99.94%
    PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
    PKI(5-24)
  • HY-W012980
    Isovaleric acid
    Activator ≥98.0%
    Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders.
    Isovaleric acid
  • HY-N1420
    Rhamnose
    Inducer ≥98.0%
    Rhamnose (L-Rhamnose) is an orally active deoxysugar that is widely found in plants and bacteria. Rhamnose can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models, showing anti-aging effects. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose is also used in cancer research.
    Rhamnose
  • HY-B1898
    Metadoxine
    99.88%
    Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
    Metadoxine
  • HY-N2118
    Bilobetin
    Activator 99.39%
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
    Bilobetin
  • HY-12659
    LX7101
    Inhibitor 99.54%
    LX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research.
    LX7101
  • HY-18991
    CCG215022
    Inhibitor 98.69%
    CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
    CCG215022
  • HY-100984
    HA-100
    Inhibitor 99.80%
    HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.
    HA-100
  • HY-153967
    BLU0588
    Inhibitor
    BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research.
    BLU0588
  • HY-150076
    BLU2864
    Inhibitor 99.24%
    BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research.
    BLU2864
  • HY-12059A
    AT7867 dihydrochloride
    Inhibitor 99.75%
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
    AT7867 dihydrochloride
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