ROCK

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1049 Y-27632 2HCl 14 mg/mL 64 mg/mL '<1 mg/mL
S1459 Thiazovivin <1 mg/mL 15 mg/mL <1 mg/mL
S1573 Fasudil (HA-1077) HCl 65 mg/mL 5 mg/mL '<1 mg/mL
S1474 GSK429286A <1 mg/mL 87 mg/mL 4 mg/mL
S7195 RKI-1447 <1 mg/mL 65 mg/mL <1 mg/mL
S6390 Y-27632 <1 mg/mL 49 mg/mL ''49 mg/mL
S6214 H-1152 dihydrochloride 78 mg/mL 78 mg/mL ''78 mg/mL
S3233 Emetine hydrochloride -1 mg/mL 100 mg/mL -1 mg/mL
S7687 GSK269962A HCl <1 mg/mL 100 mg/mL '6 mg/mL
S8226 Netarsudil (AR-13324) 2HCl 54 mg/mL 20 mg/mL 2 mg/mL
S6636 Azaindole 1 (TC-S 7001) <1 mg/mL 81 mg/mL 2 mg/mL
S7935 Y-39983 HCl 63 mg/mL 63 mg/mL '2 mg/mL
S8448 ZINC00881524 (ROCK inhibitor) <1 mg/mL 76 mg/mL 3 mg/mL
S7936 Belumosudil (KD025) <1 mg/mL 90 mg/mL ''<1 mg/mL
S8208 Hydroxyfasudil (HA-1100) HCl 60 mg/mL 68 mg/mL <1 mg/mL
S7563 AT13148 <1 mg/mL 62 mg/mL <1 mg/mL

亜型選択性的な製品

ROCK製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1049

Y-27632 2HCl

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

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.

S1573

Fasudil (HA-1077) HCl

Fasudil (HA-1077, AT-877), 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.

S1474

GSK429286A

GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

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.

S6390

Y-27632

Y-27632 is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

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.

S3233

Emetine hydrochloride

Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

S7687

GSK269962A HCl

GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

S8226

Netarsudil (AR-13324) 2HCl

Netarsudil (a.k.a. AR-13324) is 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.

S6636

Azaindole 1 (TC-S 7001)

Azaindole 1 (TC-S 7001) 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.

S7935

Y-39983 HCl

Y-39983 HCl (Y-33075) is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.

S8448

ZINC00881524 (ROCK inhibitor)

ZINC00881524 is a ROCK inhibitor.

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.

S8208

Hydroxyfasudil (HA-1100) HCl

Hydroxyfasudil (HA-1100), 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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1049

Y-27632 2HCl

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

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.

S1573

Fasudil (HA-1077) HCl

Fasudil (HA-1077, AT-877), 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.

S1474

GSK429286A

GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

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.

S6390

Y-27632

Y-27632 is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

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.

S3233

Emetine hydrochloride

Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

S7687

GSK269962A HCl

GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

S8226

Netarsudil (AR-13324) 2HCl

Netarsudil (a.k.a. AR-13324) is 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.

S6636

Azaindole 1 (TC-S 7001)

Azaindole 1 (TC-S 7001) 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.

S7935

Y-39983 HCl

Y-39983 HCl (Y-33075) is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.

S8448

ZINC00881524 (ROCK inhibitor)

ZINC00881524 is a ROCK inhibitor.

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.

S8208

Hydroxyfasudil (HA-1100) HCl

Hydroxyfasudil (HA-1100), 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.

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.

Tags: ROCK inhibition | ROCK activity | ROCK activation | Rho kinase inhibition | Rho kinase activation | Rho kinase activity | ROCK phosphorylation | ROCK signaling pathway | Rho kinase assay | Rho kinase signaling pathway | ROCK inhibitors for glaucoma | ROCK inhibitor review