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
|
|
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.This product is not soluble in saline. Please do not dissolve it in saline for administration. |
-
Eye Vis (Lond), 2024, 11(1):37
-
PLoS Pathog, 2023, 19(3):e1011295
-
Ren Fail, 2023, 45(1):2172961
|
|
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. |
-
Nat Commun, 2024, 15(1):840
-
Nat Commun, 2024, 15(1):1300
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00103-4
|
|
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. |
-
Redox Biol, 2024, 75:103249
-
Int J Mol Sci, 2024, 25(8)4340
-
Cell Rep, 2023, 42(7):112696
|
|
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. |
-
J Transl Med, 2024, 22(1):844
-
PLoS One, 2024, 19(9):e0309794
-
bioRxiv, 2024, 2024.05.09.593171
|
|
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 Commun, 2023, 14(1):3543
-
Nat Commun, 2023, 14(1):3543
-
Oncogene, 2023, 42(39):2878-2891
|
|
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). |
-
Pathogens, 2023, 12(6)845
-
Pathogens, 2023, 12(6)845
-
Prostate, 2023, 10.1002/pros.24632
|
|
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
|
|
S6507 |
KN-92 phosphate
|
KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII). |
-
Sci Rep, 2023, 13(1):5827
-
Elife, 2022, 11e74519
-
Front Physiol, 2021, 12:736920
|
|
E2202 |
1-Naphthyl PP1 hydrochloride
|
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 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. |
|
|
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. |
|
|
S6383 |
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. |
-
J Cell Biol, 2024, 223(11)e202403165
|
|
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). |
-
Eur J Pharmacol, 2024, S0014-2999(24)00322-4
|
|
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
|
|
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.This product is not soluble in saline. Please do not dissolve it in saline for administration. |
- Eye Vis (Lond), 2024, 11(1):37
- PLoS Pathog, 2023, 19(3):e1011295
- Ren Fail, 2023, 45(1):2172961
|
|
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. |
- Nat Commun, 2024, 15(1):840
- Nat Commun, 2024, 15(1):1300
- EMBO Mol Med, 2024, 10.1038/s44321-024-00103-4
|
|
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. |
- Redox Biol, 2024, 75:103249
- Int J Mol Sci, 2024, 25(8)4340
- Cell Rep, 2023, 42(7):112696
|
|
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. |
- J Transl Med, 2024, 22(1):844
- PLoS One, 2024, 19(9):e0309794
- bioRxiv, 2024, 2024.05.09.593171
|
|
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 Commun, 2023, 14(1):3543
- Nat Commun, 2023, 14(1):3543
- Oncogene, 2023, 42(39):2878-2891
|
|
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
|
|
E2202 |
1-Naphthyl PP1 hydrochloride
|
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 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. |
|
|
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. |
|
|
S6383 |
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. |
- J Cell Biol, 2024, 223(11)e202403165
|
|