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ROCK

Isoform-selective Products

ROCK1 ROCK2

Signaling Pathway

ROCK Products

All (21)
ROCK Inhibitors (21)
New ROCK Products

Catalog No.	Product Name	Information	Product Use Citations
S1049	Y-27632 2HCl	Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a K_i 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, 627(8004):594-603 Nature, 2024, 628(8009):818-825 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, 10.1038/s41586-024-07260-z Nature, 2024, 628(8009):844-853 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.	Sci China Life Sci, 2024, 67(8):1549-1562 Ren Fail, 2024, 46(2):2396455 PeerJ, 2023, 11:e15494
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 K_i 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
S7995	Ripasudil hydrochloride dihydrate	Ripasudil hydrochloride dihydrate is a potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.	Elife, 2023, 12e80254 bioRxiv, 2023, 10.1101/2023.04.03.535438 FASEB J, 2022, 36(7):e22397
S7687	GSK269962A HCl	GSK269962A HCl is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.	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.
E1480	DJ4	DJ4 (EX-A7863) is a potent, selective ATP-competitive inhibitor of ROCK1/2 and MRCKα/β with IC50 of 5/50 nM and 10/100 nM respectively. It blocks stress fiber formation and inhibits migration and invasion of multiple cancer cell line
S7512^New	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 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.
E1978^New	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.
E2519	WAY-624704	WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
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.
S1049	Y-27632 2HCl	Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a K_i 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, 627(8004):594-603 Nature, 2024, 628(8009):818-825 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, 10.1038/s41586-024-07260-z Nature, 2024, 628(8009):844-853 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.	Sci China Life Sci, 2024, 67(8):1549-1562 Ren Fail, 2024, 46(2):2396455 PeerJ, 2023, 11:e15494
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 K_i 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
S7995	Ripasudil hydrochloride dihydrate	Ripasudil hydrochloride dihydrate is a potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.	Elife, 2023, 12e80254 bioRxiv, 2023, 10.1101/2023.04.03.535438 FASEB J, 2022, 36(7):e22397
S7687	GSK269962A HCl	GSK269962A HCl is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.	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.
E1480	DJ4	DJ4 (EX-A7863) is a potent, selective ATP-competitive inhibitor of ROCK1/2 and MRCKα/β with IC50 of 5/50 nM and 10/100 nM respectively. It blocks stress fiber formation and inhibits migration and invasion of multiple cancer cell line
S7512^New	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 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.
E1978^New	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.
E2519	WAY-624704	WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
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.
S7512^New	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.
E1978^New	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.

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