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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2155 |
Thiazovivin
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Thiazovivin 是一种ROCK 抑制剂,能提高 iPSC 的生成效率,对人胚胎干细胞具有保护作用。 | |||
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。 | |||
T7885 |
Afuresertib hydrochloride
|
ROCK; Akt; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
Afuresertib hydrochloride 是一个口服有效的,ATP 竞争性的选择性泛Akt 抑制剂,作用于Akt1、Akt2和Akt3,Ki 值分别为 0.08、2和 2.6 nM。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T14989 |
CMPD101
|
ROCK; GRK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells |
CMPD101 是膜透性的 GRK2/3高选择性小分子抑制剂,IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小,IC50值分别为 3.1 μM,2.3 μM,1.4 μM 和 8.1 μM,可研究心衰疾病。 | |||
T15798 |
LX7101
|
ROCK; LIM Kinase; PKA | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells; Tyrosine Kinase/Adaptors |
LX7101是 LIMK 和ROCK2高效抑制剂,对LIMK1/2、ROCK、PKA 的IC50分别为24、1.6、10 和小于1 nM。 | |||
T7648 |
HA-100
|
Myosin; PKA; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
HA-100 是蛋白激酶和ROCK 抑制剂,抑制PKG,PKA,PKC 和MLC 激酶的IC50值分别为 4、8、12 和 240 μM。 | |||
T4095 |
ZINC00881524
ROCK inhibitor |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
ZINC00881524 (ROCK inhibitor)是一种特异性有效 ROCK 抑制剂。 | |||
T12747 |
ROCK2-IN-2
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
ROCK2-IN-2 是 ROCK2 的特异性抑制剂(IC50 <1 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。 | |||
T1870 |
Y-27632
|
ROCK; Apoptosis | Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Y-27632 是一种 ROCK-I 和 ROCK-II 抑制剂,具有口服有效性、ATP 竞争性。Y-27632 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。 | |||
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。 | |||
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。 | |||
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。 | |||
T1911 |
Afuresertib
GSK2110183C,GSK2110183 |
ROCK; Akt; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
Afuresertib (GSK2110183) 是一个选择性,ATP 竞争性,口服有效的泛 Akt 抑制剂,作用于 Akt1、Akt2和 Akt3,Ki 值分别为 0.08、2、2.6 nM。 | |||
T7764 |
CCG-222740
|
ROCK; Rho; Ras | Cell Cycle/Checkpoint; Cytoskeletal Signaling; GPCR/G Protein; MAPK; Stem Cells |
CCG-222740 是一种口服有效的选择性Rho/MRTF 途径抑制剂。它也是 α-平滑肌的肌动蛋白表达抑制剂,可减少皮肤纤维化并阻止黑色素瘤转移。 | |||
T2011 |
RKI1313
RKI 1313,RKI-1313 |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
RKI1313 (RKI-1313) 是一种选择性抑制剂,可抑制 ROCK 依赖性信号传导、细胞骨架变化、不依赖锚定的集落形成、迁移和侵袭。 | |||
T13384L |
Y-33075 dihydrochloride
|
CaMK; ROCK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Neuroscience; Stem Cells |
Y-33075 dihydrochloride 是一种选择性ROCK 抑制剂,IC50为 3.6 nM。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T7552 |
H-1152
|
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
H-1152 是一种膜通透的选择性ROCK 抑制剂,Ki 为 1.6 nM,对ROCK2的IC50为 12 nM。 | |||
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。 | |||
T10358 |
Netarsudil Dihydrochloride
AR-13324 Dihydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) 是 Rho 相关蛋白激酶 (ROCK) 和去甲肾上腺素转运蛋白 (NET) 的抑制剂,可有效降低眼压 (IOP)。 | |||
T35328 |
H-1152 dihydrochloride
H-1152 2HCl,H-1152 dihydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
H-1152 dihydrochloride (H-1152 2HCl) 是 Rho 相关蛋白激酶 (ROCK) 的特异性抑制剂,IC50 为 12 nM,Ki 为 1.6 nM。 H-1152 dihydrochloride 抑制 PKA、PKC、PKG、Aurora A 和 CaMKII,IC50 值分别为 3.03 μM、5.68 μM、0.360 μM、0.745 μM 和 0.180 μM。 | |||
T10358L2 |
Netarsudil mesylate
AR-13324 (mesylate) |
Others | Others |
Netarsudil mesylate is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IOP) reduction. | |||
T28608 | ROCKII-IN-DI | ||
ROCKII-IN-DI is a potent, competitive inhibitor of Rho-associated coiled-coil-containing protein kinase 2 (ROCKII). | |||
T28469 |
PT-262
PT 262 |
||
PT-262 is a ROCK (Rho-associated coiled-coil forming protein kinase) inhibitor. It induces cytoskeleton remodeling and migration inhibition in lung carcinoma cells. | |||
T71120 | AR-13503 | ||
AR-13503, is an metabolite of Netarsudil (AR-11324), is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. | |||
T26821 | BIPM | ||
BIPM is a potent inhibitor of Rho-associated protein kinase 2 (ROCK2). Exposure of SH-SY5Y cells to BIPM led to significant changes in cell migration, actin stress fibers and neurite length. BIPM significantly inhibits phosphorylation of cofilin, a regula | |||
T35459 |
Glycyl H-1152 hydrochloride
|
||
Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits bett... | |||
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0183 |
Narciclasine
水仙环素,Lycoricidinol |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Narciclasine (Lycoricidinol) 是一种植物生长调节剂。它通过调节Rho/Rho 激酶/LIM 激酶/cofilin 信号传导途径,大大增加GTP 酶RhoA 活性以及以RhoA 依赖性方式诱导肌动蛋白应力纤维形成。 |