Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| M2475 | Bucladesine Sodium Salt | Bucladesine, a membrane permeable selective activator of PKA, has a critical role in up-regulation of ChAT and VAChT gene expression in PC12 cells by activation of extracellular signal regulated kinase (ERK) in Ca2+- and PKA-dependent manner. |
| M11266 | Metadoxine | Metadoxine blocks adipocyte differentiation by blocking the protein kinase A-camp response prime-binding protein (PKA-CREb) pathway. |
| M11265 | Kemptide | Kemptide is a synthetic heptapeptide that acts as a specific substrate for camp-dependent protein kinase (PKA). |
| M9782 | Bucladesine calcium | Bucladesine calcium is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. |
| M8923 | CCG215022 | CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50 values of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively. |
| M7877 | KT 5720 | KT 5720 is a specific, reversible, ATP-competitive, cell-permeable protein kinase A (PKA) inhibitor with an IC50 value of 3.3 μM, which effectively reverses MDR1-mediated multidrug resistance and reduces excitability of dorsal root ganglion (DRG) neurons by attenuating the activity of hyperpolarization-activated cyclic nucleotide-gated cation (HCN) channels and decreasing the intracellular Ca2+ concentration. ) neurons by reducing hyperpolarization-activated cyclic nucleotide-gated cation (HCN) channel activity and intracellular Ca2+ concentration. It can be used in the study of hematologic malignancies and diseases associated with HCN and DRG neurons. |
| M7870 | KT5823 | KT5823 is a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. |
| M7590 | A3 hydrochloride | A-3 Hydrochloride is A potent, cellular permeable, reversible, atP-competitive, non-selective antagonist targeting multiple kinases. A-3 Hydrochloride is an inhibitor of PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM), and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibited PKC and casein kinase I activity with Ki of 47 µM and 80 µM, respectively. |
| M6552 | C-1 (HA-100) | Ha-100 is a potent protein kinase inhibitor with IC50 values of 4 μM, 8 μM, 12 μM and 240 μM against PKG, PKA, PKC and MLC kinases, respectively. Ha-100 is also used as a ROCK inhibitor. |
| M6291 | 5-Iodotubercidin | 5-IOdotubercidin (NSC 113939), an ATP analogue, is a potent inhibitor of adenosine kinase with an IC50 value of 26 nM. 5-IOdotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by activating phosphorylase and glycogen synthase. 5-IOdotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin inhibitors. |
| M3559 | H-89 | H-89 is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
| M1729 | H-89 Dihydrochloride | H-89 dihydrochloride is a selective inhibitor of protein kinase A (PKA) with an IC50 value of 135 nM. |
| M1593 | 8-Bromo-cAMP | 8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator. |
| M43559 | BLU0588 | 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. |
| M42037 | HA-1004 | HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. |
| M30532 | Sp-cAMPS | Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM. |
| M30406 | Balanol | Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides. |
| M28584 | STAD 2 | STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism. |
| M28396 | Sp-cAMPS sodium salt | Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM. |
| M27857 | 8-pCPT-2'-O-Me-cAMP-AM | 8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway. |
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