Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3518 |
GSK269962A
GSK269962B,GSK 269962,GSK269962A HCl |
ROCK; S6 Kinase | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
GSK269962A (GSK269962A HCl) 是一种有效的ROCK 抑制剂,具有抗炎和血管舒张作用。它作用于重组人ROCK1和ROCK2,IC50分别为 1.6 和 4 nM。 | |||
T12746 |
ROCK inhibitor-2
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
ROCK inhibitor-2 是一种 ROCK1和 ROCK2的选择性双重抑制剂,IC50值分别为 17 nM 和2 nM。 | |||
T2633 |
GSK429286A
RHO-15 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
GSK429286A (RHO-15) 是一种选择性ROCK1/2抑制剂,IC50值为14 和 63 nM。 | |||
T9847 |
TLC2976-0103
|
||
ROCK1-IN-1 是一种ROCK1抑制剂,Ki 值为 540 nM。ROCK1-IN-1 可用于高血压、青光眼、勃起功能障碍的研究。 | |||
T14960 |
Chroman 1
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Chroman 1 是高效的的ROCK 选择性抑制剂,对 ROCK2 (IC50=1 pM) 的抑制作用强于 ROCK1 (IC50=52 pM) 。它对MRCK 也有抑制作用,IC50为 150 nM。 | |||
T27471 |
GSK299115A
GSK 299115A,GSK-299115A |
GRK | GPCR/G Protein |
GSK299115A (GSK-299115A) 是一种选择性的ROCK1抑制剂。GSK299115A 抑制ROCK1、RSK1和p70S6K 的IC50分别为8nM、620nM 和560nM。 | |||
T7301 |
BDP5290
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
BDP5290 是一种有效 ROCK 和 MRCK 抑制剂,对 ROCK1、ROCK2、MRCKα 和 MRCKβ 的 IC50 分别为 5、50 、10 和 100 nM。 | |||
T3513 |
GSK180736A
GSK180736 |
ROCK; GRK; PKA | Cell Cycle/Checkpoint; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells; Tyrosine Kinase/Adaptors |
GSK180736A 是 Rho 相关卷曲螺旋激酶 1 (ROCK1) 抑制剂,IC50值为 100 nM。它也是选择性的ATP-竞争性 G 蛋白偶联受体激酶 2 抑制剂,IC50值为 0.77 μM,其选择性比其他 GRK 高 100 倍以上。 | |||
T12721 |
Rho-Kinase-IN-1
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Rho-Kinase-IN-1 是一种 ROCK 抑制剂,对 ROCK1 和 ROCK2 的 Kis 分别为 30.5 nM 和 3.9 nM。 Rho-Kinase-IN-1 可用于细胞过度增殖、重塑、水肿和炎症疾病的研究。 | |||
T4276 |
Hydroxyfasudil Hydrochloride
Hydroxyfasudil (HA-1100) HCl,羟基法舒地尔盐酸盐,RHO-激酶抑制剂,HA 1100 hydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) 是一种ROCK 抑制剂,对ROCK1和ROCK2的IC50值分别为 0.73 和 0.72 μM。 | |||
T1898 |
RKI-1447
RKI1447 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
RKI-1447 是一种高效的ROCK1和ROCK2的小分子抑制剂,IC50值分别为14.5和6.2 nM。 | |||
T4276L |
Hydroxyfasudil
Hydroxy-Fasudil,HA-1100,羟基法舒地尔 |
ROCK; PKA | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Hydroxyfasudil (Hydroxy-Fasudil) 是一种ROCK 抑制剂,对ROCK1和ROCK2的IC50分别为 0.73 和 0.72 μM。 | |||
T11402L |
GKI-1 HCl
GKI-1 HCl( 2444764-03-6 Free base) |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
GKI-1 HCl 是 Greatwall (GWL)激酶抑制剂,对hGWLFL 和hGWL-KinDom 有抑制作用。GKI-1 HCl 对 ROCK1抑制作用较为显著。 | |||
T1606 |
Fasudil
HA-1077,AT877,法舒地尔 |
ROCK; Serine/threonin kinase; Calcium Channel; PKA; PKC; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors |
Fasudil (HA-1077) 是一种非特异性 RhoA/ROCK 抑制剂,也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用,ROCK1 的 Ki 值为 0.33 μM,ROCK2 和 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。 | |||
T27467 |
GSK270822A
GSK 270822A,GSK-270822A |
GRK | GPCR/G Protein |
GSK270822A 是一种选择性的 ROCK1抑制剂。GSK270822A 抑制 ROCK1,RSK1,p70S6K 的 IC50 分别为9nM,1100nM,1550nM。 | |||
TQ0319 |
Ripasudil
K-115,瑞舒地尔盐酸二水合物,Ripasudil hydrochloride dihydrate |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Ripasudil (Ripasudil hydrochloride dihydrate) 是一种 ROCK 特异性抑制剂,能够抑制 ROCK1和 ROCK2的活性,IC50值分别为 51 和 19 nM。 | |||
T3060 |
Fasudil hydrochloride
Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877 |
ROCK; Serine/threonin kinase; Calcium Channel; HIV Protease; PKA; PKC; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors |
Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂,也抑制蛋白激酶,对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。 | |||
T60924 |
Verosudil
AR-12286 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Verosudil (AR-12286) 是一种高效的 Rho 激酶 (ROCK) 抑制剂,对 ROCK1 和 ROCK2 的 Ki 分别为 2 和 2 nM。AR-12286 可逆转类固醇诱导的小鼠眼内压,可通过增加眼房水通过小梁网流出来减缓眼压。 | |||
T11402 |
GKI-1
|
Others | Others |
GKI-1是 Greatwall (GWL)激酶抑制剂,对 hGWLFL 具有抑制,其 IC50为4.9。GKI-1对 hGWL-KinDom 也具有抑制作用,其 IC50 为 2.5 µM。GKI-1 对 ROCK1抑制效果比 hGWLFL 和hGWL-KinDom 好,其IC50为11 µM, 仅微弱抑制 PKA。 | |||
T6867 |
Belumosudil
KD025,Rezurock,ROCK inhibitor,SLx-2119 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Belumosudil (Rezurock) 是一种选择性的ROCK2抑制剂,对 ROCK1 和 ROCK2 的IC50值分别为 24 µM 和 105 nM,具有抗纤维化作用。 | |||
T22037 |
AS 1892802
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
AS 1892802是一种强效和选择性的ROCK 抑制剂。AS 1892802 用于人ROCK2、大鼠ROCK2和人ROCK1的 IC50值分别为52nM、57nM 和122nM。AS 1892802的镇痛作用起效速度与曲马多和双氯芬酸的起效速度一样快。 | |||
T1828 |
TTP 22
|
Casein Kinase | Metabolism; Stem Cells |
TTP 22 是一种高亲和力、ATP 竞争性酪蛋白激酶 2 抑制剂,IC50和 Ki 值分别为 0.1 uM 和 40 nM。 | |||
T4488 |
GSK-25
GSK25 |
ROCK; S6 Kinase; mTOR | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
GSK-25 是一种选择性的,具有口服活性的 ROCK1抑制剂。它对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性,RSK1的 IC50 为 398 nM,p70S6K 的 IC50 为 1000nM。它可抑制 P450,对 CYP2C9、CYP2D6和 CYP3A4的 IC50分别为2.5、5.2和2.5 μM。 | |||
T16855 | SB-772077B dihydrochloride | ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively). | |||
T39555 |
Belumosudil mesylate
SLx-2119mesylate,KD025 mesylate |
||
Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC 50 s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties. | |||
T7391 |
SAR407899
|
ROCK; Rho | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SAR407899 是一种选择性的 ATP 竞争性ROCK 抑制剂,对ROCK-2的IC50值为 135 nM,对人和大鼠ROCK-2的Ki 值分别为 36 和 41 nM。它是 Rho 激酶抑制剂,有效抑制 endothelin-1 诱导的肾阻力动脉收缩。 | |||
T39944 |
HSD1590
|
||
HSD1590 is a highly effective and potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.22 nM and 0.51 nM, respectively. It demonstrates exceptional binding affinity to ROCK, with Kd values below 2 nM. Moreover, HSD1590 showcases minimal cytotoxicity, making it an ideal compound for various applications. | |||
T39519 |
GSK269962A hydrochloride
GSK 269962 hydrochloride |
||
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a highly potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively, for recombinant human isoforms. This compound exhibits both anti-inflammatory and vasodilatory properties. | |||
T74808 | THK01 | ||
THK01 是一种有效的 ROCK2抑制剂,对 ROCK2和 ROCK1的 IC50值分别为 5.7 和 923 nM。THK01 通过 ROCK2-STAT3 信号通路抑制乳腺癌转移。THK01 可用于乳腺癌研究。 | |||
T23308 |
SAR407899 hydrochloride
6-(哌啶-4-氧基)异喹啉-1(2H)-酮盐酸盐 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SAR407899 hydrochloride 是一种选择性,ATP 竞争性的ROCK 抑制剂,对人和大鼠ROCK2的Ki 值分别为 36 和 41 nM,对ROCK2的IC50值为 135 nM。 | |||
T10275 |
AKT-IN-3
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1 | |||
T61905 |
RKI-1447 dihydrochloride
|
||
RKI 1447 dihydrochloride 是一种有效的,选择性的 ROCK 抑制剂(ROCK1 IC50=14.5 nM,ROCK2 IC50 = 6.2 nM)。RKI 1447 dihydrochloride 对结直肠癌细胞的生长具有抑制作用,并促进其凋亡。 | |||
TQ0187 |
SR-3677
|
ROCK; Autophagy | Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
SR-3677 是一种有效且特异性的 ROCK2 抑制剂,IC50值为3 nM。 | |||
T1725 |
Y-27632 dihydrochloride
反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐,Y-27632 2HCl |
ROCK; Apoptosis | Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂,具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。 | |||
TQ0110 |
ROCK-IN-2
TC-S 7001,Azaindole 1 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
ROCK-IN-2 (Azaindole 1) 是一种选择性,ATP-竞争型的ROCK 抑制剂,对ROCK-1和ROCK-2的IC50值分别为 0.6 和 1.1 nM。 | |||
T63506 | Chroman 1 dihydrochloride | ||
Chroman 1 dihydrochloride 是选择性的 ROCK 高效抑制剂,对 ROCK2 (IC50: 1 pM) 的作用比 ROCK1 (IC50: 52 pM) 更强,也能够抑制 MRCK 的活性 (IC50: 150 nM)。 | |||
T61382 |
Fasudil dihydrochloride
|
||
Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3]. | |||
T7492 |
Ripasudil free base
K-115 (free base) |
ROCK; Antibacterial | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Microbiology/Virology; Stem Cells |
Ripasudil free base (K-115 (free base)) 是一种ROCK 特异性抑制剂,能够抑制ROCK1和ROCK2的活性,IC50值分别为 51 和 19 nM。 | |||
T71119 |
Netarsudil free base
|
||
Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudi... | |||
T2482 |
AT13148
|
ROCK; SGK; Akt; PKA; S6 Kinase | Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
AT13148 是一种 ATP 竞争性 AGC 激酶口服抑制剂,能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性,IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。 | |||
T39733 |
Hu7691 free base
|
||
Hu7691 free base is an orally active, selective Akt inhibitor. It exhibits IC50 values of 4.0 nM, 97.5 nM, and 28 nM for Akt1, Akt2, and Akt3, respectively. Furthermore, it effectively inhibits tumor growth and facilitates a reduction in cutaneous toxicity in mice. | |||
T15428 |
Uprosertib hydrochloride
GSK2141795 (hydrochloride) |
Others | Others |
Uprosertib hydrochloride is a potent and selective inhibitor of pan-Akt (IC50: 180/328/38 nM for Akt1/Akt2/Akt3, respectively). | |||
T39899 | Hu7691 | Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Hu7691 是一种具有口服活性、选择性和高效性的 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3,抑制神经母细胞瘤细胞增殖,诱导神经母细胞瘤细胞的分化。 |