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) | ||
|---|---|---|---|---|
| 水 | 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 |
| S3239 | Emetine Dihydrochloride | -1 mg/mL | 100 mg/mL | '''-1 mg/mL |
| S6636 | Azaindole 1 (TC-S 7001) | <1 mg/mL | 81 mg/mL | 2 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 |
| 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 | KD025 (SLx-2119) | <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 2HClY-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. |
The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
|
|
| S1459 |
ThiazovivinThiazovivin 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) HClFasudil(HA-1077), 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. |
The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
|
| S1474 |
GSK429286AGSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
ROCK antagonists interfere with infection-induced changes in cell shape, but do not reduce HCMV yield. (A) ROCK antagonists block actin reorganization after infection. Fibroblasts were treated with solvent (DMSO) or drug (10 uM Y27632 or 140 nM GSK429286A) beginning 1 h after mock infection or infection with WT virus. Cells received fresh medium containing solvent or drug every 24 h. Cultures were assayed for actin using labeled phalloidin (red), pUL37 (green), and DNA (blue). (B) ROCK antagonist blocks cell rounding at 24 hpi. Fibroblasts were treated with solvent or drug beginning 1 h after mock infection or infection with WT virus. Cultures received fresh medium with drug every 24 h and were analyzed by treatment with 5 μM fluorophore calcein red-orange AM for 1 h, followed by spinning disk confocal Z-stack live cell imaging and reconstruction of 3D images. (C) ROCK activity does not influence virus yield. Fibroblasts were treated with solvent or ROCK antagonists beginning 1 h after infection with WT HCMV. Cultures received fresh medium with drug every 24 h, and extracellular virus yields were determined by plaque assay. |
|
| S7195 |
RKI-1447RKI-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. |
(d) ROCK inhibition blocks CC-RCC migration in a transwell assay. RCC10 or 786-O cells were treated with Y-27632, RKI 1447 or DMSO vehicle (as indicated) for 6 h. The assay was performed in duplicate and the experiment was repeated three times. Statistical analysis in (b-d) was performed using a paired t-test comparing each normalized dose to the negative control (*P<0.05, **P<0.01 and ***P<0.001); s.e.m.'s are shown.
|
|
| S3239新 |
Emetine DihydrochlorideEmetine Dihydrochloride, 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 Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect. |
||
| S6636新 |
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. |
||
| S7687 |
GSK269962A HClGSK269962 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) 2HClNetarsudil (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. |
||
| S7935 |
Y-39983 HClY-39983 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 |
KD025 (SLx-2119)KD025 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) HClHydroxyfasudil (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 |
AT13148AT13148 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. |
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
|
| 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 2HClY-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. |
The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
|
|
| S1459 |
ThiazovivinThiazovivin 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) HClFasudil(HA-1077), 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. |
The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
|
| S1474 |
GSK429286AGSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
ROCK antagonists interfere with infection-induced changes in cell shape, but do not reduce HCMV yield. (A) ROCK antagonists block actin reorganization after infection. Fibroblasts were treated with solvent (DMSO) or drug (10 uM Y27632 or 140 nM GSK429286A) beginning 1 h after mock infection or infection with WT virus. Cells received fresh medium containing solvent or drug every 24 h. Cultures were assayed for actin using labeled phalloidin (red), pUL37 (green), and DNA (blue). (B) ROCK antagonist blocks cell rounding at 24 hpi. Fibroblasts were treated with solvent or drug beginning 1 h after mock infection or infection with WT virus. Cultures received fresh medium with drug every 24 h and were analyzed by treatment with 5 μM fluorophore calcein red-orange AM for 1 h, followed by spinning disk confocal Z-stack live cell imaging and reconstruction of 3D images. (C) ROCK activity does not influence virus yield. Fibroblasts were treated with solvent or ROCK antagonists beginning 1 h after infection with WT HCMV. Cultures received fresh medium with drug every 24 h, and extracellular virus yields were determined by plaque assay. |
|
| S7195 |
RKI-1447RKI-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. |
(d) ROCK inhibition blocks CC-RCC migration in a transwell assay. RCC10 or 786-O cells were treated with Y-27632, RKI 1447 or DMSO vehicle (as indicated) for 6 h. The assay was performed in duplicate and the experiment was repeated three times. Statistical analysis in (b-d) was performed using a paired t-test comparing each normalized dose to the negative control (*P<0.05, **P<0.01 and ***P<0.001); s.e.m.'s are shown.
|
|
| S3239新 |
Emetine DihydrochlorideEmetine Dihydrochloride, 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 Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect. |
||
| S6636新 |
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. |
||
| S7687 |
GSK269962A HClGSK269962 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) 2HClNetarsudil (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. |
||
| S7935 |
Y-39983 HClY-39983 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 |
KD025 (SLx-2119)KD025 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) HClHydroxyfasudil (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 |
AT13148AT13148 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. |
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
|
