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PKA
T0465 Ellagic acid Ellagic acid 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.
T0610 Piceatannol Piceatannol 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.
T1418 Bucladesine sodium salt Bucladesine, PKA activator, is a cyclic nucleotide derivative that mimics the action of endogenous cAMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant.
T1606 Fasudil Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
T1837 BX-912 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.
T2205 Theophylline-7-acetic acid 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
T2356 Ro 3306 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.
T2482 AT13148 AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
T2851 Daphnetin Daphnetin, 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.
T3050 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.
T3060 Fasudil (HA-1077) hydrochloride Fasudil Hydrochloride 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.
T3498 CCG215022 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, 5 and 1, respectively.
T3513 GSK180736A 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).
T6139 A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
T6250 H 89 diHydrochloride H 89 2 hCl is a potent inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM.
T6303 CCT128930 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.
T6304 AT7867 AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.
T6312 R547 R547 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.
T6315 MLN8054 MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
T6605 NH125 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.
T6747 8-Bromo-cAMP 8-Bromo-cAMP is a long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
T4444 A-674563 HCl (552325-73-2(free base)) 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 the CMGC, CAMK, and TK families [1].
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