S1421 |
Staurosporine (AM-2282)
|
Staurosporine (AM-2282, Antibiotic AM-2282, 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. |
-
Cancer Res, 2022, canres.0218.2021
-
Neurotherapeutics, 2022, 10.1007/s13311-022-01212-z
-
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
|
|
S2642 |
1-Naphthyl PP1(1-NA-PP1)
|
1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
|
|
S6214New |
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. |
|
|
S6383New |
1-NM-PP1
|
1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. |
|
|
S6787 |
KN-93
|
KN-93 is a cell-permeable, reversible and competitive inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II) with Ki of 2.58 μM at rabbit myocardial CaM kinase activity. |
-
Nutr Neurosci, 2022, 1-19
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00135-1
-
Oncogene, 2021, 10.1038/s41388-020-01628-x
|
|
S7188 |
CID755673
|
CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.
|
-
Nat Cell Biol, 2019, 21(6):778-790
-
Cancer Res, 2018, 78(18):5274-5286
-
Aging (Albany NY), 2018, 10(12):3736-3744
|
|
S7422 |
KN-62
|
KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM; also a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM). It is selective for CaMKII relative to PKA, PKC and MLCK, but inhibits CaMKI and CaMKIV equally well, The Ki value of KN-62 for CaMK V is 0.8 μM. |
-
Transl Vis Sci Technol, 2022, 11(4):4
-
Nat Commun, 2021, 12(1):3519
-
Autophagy, 2021, 1-19
|
|
S7423 |
KN-93 Phosphate
|
KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy. |
-
EMBO Rep, 2022, e53373
-
Commun Biol, 2022, 5(1):96
-
Nutr Neurosci, 2022, 1-19
|
|
S7436 |
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. |
-
Acta Pharmacol Sin, 2018, 10.1038/s41401-018-0165-9
-
Drug Des Devel Ther, 2018, Drug Des Devel Ther
-
BMC Cancer, 2016, 16(1):813
|
|
S8274 |
STO-609
|
STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy. |
-
EMBO Rep, 2022, e53373
-
Cell Res, 2021, 10.1038/s41422-021-00565-y
-
Autophagy, 2021, 1-14
|
|
S6221 |
Methyl cinnamate
|
Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes. |
|
|
S3609 |
Berbamine dihydrochloride
|
Berbamine (BA, BBM) dihydrochloride, a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA, BBM) dihydrochloride induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). |
|
|
S9141 |
Berbamine
|
Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA) induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). |
-
Onco Targets Ther, 2019, 12:11437-11451
|
|
S6507 |
KN-92 phosphate
|
KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII). |
-
Front Physiol, 2021, 12:736920
|
|
S1421 |
Staurosporine (AM-2282)
|
Staurosporine (AM-2282, Antibiotic AM-2282, 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. |
- Cancer Res, 2022, canres.0218.2021
- Neurotherapeutics, 2022, 10.1007/s13311-022-01212-z
- Anal Chem, 2022, 10.1021/acs.analchem.1c05455
|
|
S2642 |
1-Naphthyl PP1(1-NA-PP1)
|
1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
|
|
S6214New |
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. |
|
|
S6383New |
1-NM-PP1
|
1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. |
|
|
S6787 |
KN-93
|
KN-93 is a cell-permeable, reversible and competitive inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II) with Ki of 2.58 μM at rabbit myocardial CaM kinase activity. |
- Nutr Neurosci, 2022, 1-19
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00135-1
- Oncogene, 2021, 10.1038/s41388-020-01628-x
|
|
S7188 |
CID755673
|
CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.
|
- Nat Cell Biol, 2019, 21(6):778-790
- Cancer Res, 2018, 78(18):5274-5286
- Aging (Albany NY), 2018, 10(12):3736-3744
|
|
S7422 |
KN-62
|
KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM; also a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM). It is selective for CaMKII relative to PKA, PKC and MLCK, but inhibits CaMKI and CaMKIV equally well, The Ki value of KN-62 for CaMK V is 0.8 μM. |
- Transl Vis Sci Technol, 2022, 11(4):4
- Nat Commun, 2021, 12(1):3519
- Autophagy, 2021, 1-19
|
|
S7423 |
KN-93 Phosphate
|
KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy. |
- EMBO Rep, 2022, e53373
- Commun Biol, 2022, 5(1):96
- Nutr Neurosci, 2022, 1-19
|
|
S7436 |
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. |
- Acta Pharmacol Sin, 2018, 10.1038/s41401-018-0165-9
- Drug Des Devel Ther, 2018, Drug Des Devel Ther
- BMC Cancer, 2016, 16(1):813
|
|
S8274 |
STO-609
|
STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy. |
- EMBO Rep, 2022, e53373
- Cell Res, 2021, 10.1038/s41422-021-00565-y
- Autophagy, 2021, 1-14
|
|