S1582 |
H 89 2HCl
|
H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy. |
-
Nat Commun, 2024, 15(1):8887
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
|
|
S1421 |
Staurosporine (STS)
|
Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
-
Nat Commun, 2024, 15(1):489
-
Nat Commun, 2024, 15(1):3816
-
Nat Commun, 2024, 15(1):3816
|
|
S1113 |
GSK690693
|
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
-
EMBO J, 2024, 10.1038/s44318-024-00244-9
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
-
CNS Neurosci Ther, 2024, 30(8):e14913
|
|
S1573 |
Fasudil HCl
|
Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Sci China Life Sci, 2024, 67(8):1549-1562
-
CNS Neurosci Ther, 2024, 30(11):e70098
|
|
S7858 |
Dibutyryl-cAMP (Bucladesine)
|
Dibutyryl-cAMP (Bucladesine, dbcAMP) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor. |
-
Cell Rep Med, 2024, 5(3):101477
-
ACS Appl Mater Interfaces, 2024, 16(40):54292-54303
-
Commun Biol, 2024, 7(1):1393
|
|
S2670 |
A-674563 HCl
|
A-674563 HCl is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC. |
-
J Biol Chem, 2024, 300(2):105641
-
Nat Commun, 2023, 14(1):886
-
Exp Gerontol, 2023, 173:112091
|
|
S7857 |
8-Bromo-cAMP
|
8-bromo-cAMP (8-Br-Camp) is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM; and a PKA activator. |
-
Stem Cell Res Ther, 2024, 15(1):438
-
Biomed Pharmacother, 2024, 176:116858
-
J Transl Med, 2024, 22(1):478
|
|
S8388 |
ML-7 HCl
|
ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively. |
-
J Tradit Chin Med, 2024, 44(5):885-895
-
Sci Adv, 2024, 10(44):eadp0631
-
Ecotoxicol Environ Saf, 2023, 257:114940
|
|
S7563 |
AT13148
|
AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 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. Phase 1.
|
-
Neoplasia, 2023, 10.1016/j.neo.2023.100948
-
Cancers (Basel), 2022, 14(23)5943
-
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
|
|
S2554 |
Daphnetin
|
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities. |
-
Sci Rep, 2021, 11(1):11491
-
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
-
Int Immunopharmacol, 2019, 72:195-203
|
|
S0754 |
Bisindolylmaleimide IV
|
Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM. |
-
Elife, 2021, 10e68473
|
|
E4793New |
Bucladesine calcium
|
Bucladesine calcium (Dibutyryl-cAMP Calcium Salt, DBcAMP calcium salt) is a cell-permeable analog of cyclic AMP. It serves as a potent activator of protein kinase A (PKA) and mimics the effects of endogenous cAMP. It also inhibits phosphodiesterase (PDE) activity, with the potential to treat congestive heart failure, wound healing, and inflammation. |
|
|
E2506 |
A-3 hydrochloride
|
A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively. |
|
|
S6214 |
H-1152 dihydrochloride
|
H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. |
|
|
S2964 |
HA-100 dihydrochloride
|
HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively. |
-
Adv Sci (Weinh), 2024, 11(4):e2304987
|
|
S1582 |
H 89 2HCl
|
H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy. |
- Nat Commun, 2024, 15(1):8887
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
|
|
S1421 |
Staurosporine (STS)
|
Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
- Nat Commun, 2024, 15(1):489
- Nat Commun, 2024, 15(1):3816
- Nat Commun, 2024, 15(1):3816
|
|
S1113 |
GSK690693
|
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
- EMBO J, 2024, 10.1038/s44318-024-00244-9
- EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
- CNS Neurosci Ther, 2024, 30(8):e14913
|
|
S1573 |
Fasudil HCl
|
Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
- J Immunother Cancer, 2024, 12(11)e009805
- Sci China Life Sci, 2024, 67(8):1549-1562
- CNS Neurosci Ther, 2024, 30(11):e70098
|
|
S2670 |
A-674563 HCl
|
A-674563 HCl is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC. |
- J Biol Chem, 2024, 300(2):105641
- Nat Commun, 2023, 14(1):886
- Exp Gerontol, 2023, 173:112091
|
|
S8388 |
ML-7 HCl
|
ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively. |
- J Tradit Chin Med, 2024, 44(5):885-895
- Sci Adv, 2024, 10(44):eadp0631
- Ecotoxicol Environ Saf, 2023, 257:114940
|
|
S7563 |
AT13148
|
AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 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. Phase 1.
|
- Neoplasia, 2023, 10.1016/j.neo.2023.100948
- Cancers (Basel), 2022, 14(23)5943
- Br J Cancer, 2021, 10.1038/s41416-021-01442-6
|
|
S2554 |
Daphnetin
|
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities. |
- Sci Rep, 2021, 11(1):11491
- Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
- Int Immunopharmacol, 2019, 72:195-203
|
|
S0754 |
Bisindolylmaleimide IV
|
Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM. |
- Elife, 2021, 10e68473
|
|
S6214 |
H-1152 dihydrochloride
|
H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. |
|
|
S2964 |
HA-100 dihydrochloride
|
HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively. |
- Adv Sci (Weinh), 2024, 11(4):e2304987
|
|