S1049 |
Y-27632 2HCl
|
Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における Ki は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。 |
-
Neural Regen Res, 2025, 20(1):242-252
-
Nature, 2024, 627(8004):594-603
-
Nature, 2024, 628(8009):818-825
|
|
S6390 |
Y-27632
|
Y-27632 is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. |
-
Nature, 2024, 628(8009):844-853
-
Nature, 2024, 10.1038/s41586-024-07260-z
-
Science, 2024, 383(6687):eadi7342
|
|
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
|
|
S1459 |
Thiazovivin
|
Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation. |
-
Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7
-
Nat Commun, 2024, 15(1):7186
-
Nucleic Acids Res, 2024, gkae158
|
|
S1474 |
GSK429286A
|
GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
-
iScience, 2023, 26(12):108532
-
Sci Rep, 2022, 12(1):7
-
Cancer Sci, 2020, 112(1):133-143
|
|
S8448 |
ZINC00881524 (ROCK inhibitor)
|
ZINC00881524 is a ROCK inhibitor. |
-
bioRxiv, 2023, 2023.06.07.544100
-
Nat Commun, 2022, 13(1):7171
-
Cancer Res, 2022, canres.2691.2021
|
|
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
|
|
S7195 |
RKI-1447
|
RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities. |
-
Neoplasia, 2023, 10.1016/j.neo.2023.100948
-
Sci Rep, 2022, 12(1):7
-
GCRIS, 2022,
|
|
S7936 |
Belumosudil (KD025)
|
Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2. |
-
Zool Res, 2024, 45(3):535-550
-
bioRxiv, 2024, 2024.09.16.613317
-
Commun Biol, 2023, 10.1038/s42003-023-05552-0
|
|
S7687 |
GSK269962A HCl
|
GSK269962A HClは一種の選択性的なROCK阻害剤で、ROCK1とROCK2に作用する時のIC50値が1.6nMと4nMに分かれることです。 |
-
Stem Cell Reports, 2024, 19(4):579-595
-
bioRxiv, 2024, 2024.01.09.574940
-
bioRxiv, 2024, 2024.01.09.574940
|
|
S7935 |
Y-39983 Dihydrochloride
|
Y-39983 (Y-33075) Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM. |
-
Cells, 2023, 12(9)1307
-
Cell, 2020, 182(3):685-712.e19
-
Cell, 2020, 182(3):685-712.e19
|
|
S8226 |
Netarsudil (AR-13324) 2HCl
|
Netarsudil (AR-13324) is a ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension. |
-
Int J Mol Sci, 2023, 24(6)5464
|
|
S8208 |
Hydroxyfasudil HCl
|
Hydroxyfasudil HCl, an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively. |
-
Eur J Pharmacol, 2024, 979:176835
-
bioRxiv, 2020, 10.1101/2020.11.26.393801
|
|
E1261 |
Chroman 1
|
Chroman 1 is a highly potent and selective ROCK inhibitor with IC50 of 1 pM and 52 pM against ROCK2 and ROCK1, respectively. Chroman 1 also inhibits the activity of MRCK with IC50 of 150 nM. |
|
|
S7512New |
GSK269962A
|
GSK269962A is a potent and selective inhibitor of ROCK with IC50 values of 1.6 nM for ROCK1 and 4 nM for ROCK2. It shows potential as an alternative treatment for overactive bladder (OAB), and also exhibits anti-inflammatory and vasodilatory activities. |
|
|
S6636 |
Azaindole 1 (BAY-549)
|
Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 nM and 1.1 nM for human ROCK1 and ROCK2 in an ATP-competitive manner. |
|
|
E1978New |
Zelasudil
|
Zelasudil (RXC007) is a selective inhibitor of Rho-associated coiled-coil-containing kinase 2 (ROCK2). It has been found to have the antifibrotic effect. |
|
|
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. |
|
|
E1921New |
NRL-1049
|
NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice. |
|
|
S1049 |
Y-27632 2HCl
|
Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における Ki は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。 |
- Neural Regen Res, 2025, 20(1):242-252
- Nature, 2024, 627(8004):594-603
- Nature, 2024, 628(8009):818-825
|
|
S6390 |
Y-27632
|
Y-27632 is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. |
- Nature, 2024, 628(8009):844-853
- Nature, 2024, 10.1038/s41586-024-07260-z
- Science, 2024, 383(6687):eadi7342
|
|
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
|
|
S1459 |
Thiazovivin
|
Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation. |
- Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7
- Nat Commun, 2024, 15(1):7186
- Nucleic Acids Res, 2024, gkae158
|
|
S1474 |
GSK429286A
|
GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
- iScience, 2023, 26(12):108532
- Sci Rep, 2022, 12(1):7
- Cancer Sci, 2020, 112(1):133-143
|
|
S8448 |
ZINC00881524 (ROCK inhibitor)
|
ZINC00881524 is a ROCK inhibitor. |
- bioRxiv, 2023, 2023.06.07.544100
- Nat Commun, 2022, 13(1):7171
- Cancer Res, 2022, canres.2691.2021
|
|
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
|
|
S7195 |
RKI-1447
|
RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities. |
- Neoplasia, 2023, 10.1016/j.neo.2023.100948
- Sci Rep, 2022, 12(1):7
- GCRIS, 2022,
|
|
S7936 |
Belumosudil (KD025)
|
Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2. |
- Zool Res, 2024, 45(3):535-550
- bioRxiv, 2024, 2024.09.16.613317
- Commun Biol, 2023, 10.1038/s42003-023-05552-0
|
|
S7687 |
GSK269962A HCl
|
GSK269962A HClは一種の選択性的なROCK阻害剤で、ROCK1とROCK2に作用する時のIC50値が1.6nMと4nMに分かれることです。 |
- Stem Cell Reports, 2024, 19(4):579-595
- bioRxiv, 2024, 2024.01.09.574940
- bioRxiv, 2024, 2024.01.09.574940
|
|
S7935 |
Y-39983 Dihydrochloride
|
Y-39983 (Y-33075) Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM. |
- Cells, 2023, 12(9)1307
- Cell, 2020, 182(3):685-712.e19
- Cell, 2020, 182(3):685-712.e19
|
|
S8226 |
Netarsudil (AR-13324) 2HCl
|
Netarsudil (AR-13324) is a ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension. |
- Int J Mol Sci, 2023, 24(6)5464
|
|
S8208 |
Hydroxyfasudil HCl
|
Hydroxyfasudil HCl, an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively. |
- Eur J Pharmacol, 2024, 979:176835
- bioRxiv, 2020, 10.1101/2020.11.26.393801
|
|
E1261 |
Chroman 1
|
Chroman 1 is a highly potent and selective ROCK inhibitor with IC50 of 1 pM and 52 pM against ROCK2 and ROCK1, respectively. Chroman 1 also inhibits the activity of MRCK with IC50 of 150 nM. |
|
|
S7512New |
GSK269962A
|
GSK269962A is a potent and selective inhibitor of ROCK with IC50 values of 1.6 nM for ROCK1 and 4 nM for ROCK2. It shows potential as an alternative treatment for overactive bladder (OAB), and also exhibits anti-inflammatory and vasodilatory activities. |
|
|
S6636 |
Azaindole 1 (BAY-549)
|
Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 nM and 1.1 nM for human ROCK1 and ROCK2 in an ATP-competitive manner. |
|
|
E1978New |
Zelasudil
|
Zelasudil (RXC007) is a selective inhibitor of Rho-associated coiled-coil-containing kinase 2 (ROCK2). It has been found to have the antifibrotic effect. |
|
|
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. |
|
|
E1921New |
NRL-1049
|
NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice. |
|
|