rock inhibitor-2

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。

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。

LX-7101 hydrochloride是高效的 LIMK 和 ROCK2 抑制剂，具有降压活性，抑制 LIMK1/2, ROCK, PKA，可用于研究青光眼。

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。

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。

ROCK2-IN-2 是 ROCK2 的特异性抑制剂（IC50 <1 μM）。

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。

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。

ROCK/HDAC-IN-1（Compound 10h）作为一种抑制剂，通过口服展现出对ROCK/HDAC的有效抑制。该化合物针对ROCK1/2和HDAC1/2/3/6/8表现出卓越的抑制效率，其IC50值分别为254.9 nM、58.18 nM和9.09、8.03、6.26、0.41、7.69 nM。此外，ROCK/HDAC-IN-1能激活DAMP，尤其增强了钙网蛋白（CRT）的外露和HMGB1的释放，显示其作为免疫性细胞死亡（ICD）诱导剂的潜力。对于乳腺癌细胞，特别是MDA-MB-231细胞，此抑制剂具有抗增殖活性，IC50值为0.37 μM，且能在不产生明显毒性的情况下，抑制肿瘤生长并激活T细胞。

ROCK/HDAC-IN-2 (Compound C-9) 是一种ROCK/HDAC抑制剂，对HDAC6、ROCK1和ROCK2的IC50分别为0.185 µM、0.8 µM和0.7 µM。它能够诱导癌细胞凋亡 (Apoptosis) 和线粒体膜电位变化，具备显著的抗肿瘤活性，适用于胰腺导管腺癌 (PDAC) 和三阴性乳腺癌 (TNBC) 的研究。

ROCK-IN-D2 is an effective and selective inhibitor of ROCK.

GSK429286A (RHO-15) 是一种选择性ROCK1/2抑制剂，IC50值为14 和 63 nM。

Potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively). Feng et al (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J.Med.Chem. 51 6642 PMID:18834107

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

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.

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。

Fasudil dihydrochloride（又名 HA-1077 和 AT877）是 RhoA/ROCK 的非特异性抑制剂。其对 ROCK1（Ki = 0.33 μM）、ROCK2（IC50 = 0.158 μM）、PKA（IC50 = 4.58 μM）、PKC（IC50 = 12.30 μM）及 PKG（IC50 = 1.650 μM）具有抑制作用，同时也是一种有效的钙通道阻断剂和血管扩张剂，在血管、心血管及细胞信号研究中具有多重药理研究价值。

Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1].

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。

Fasudil mesylate (HA-1077; AT877) 是一种口服有效的非特异性RhoA/ROCK抑制剂，同时能够抑制多种蛋白激酶。该化合物对ROCK1的Ki值为0.33 μM，对ROCK2、PKA、PKC和PKG的IC50值分别为0.158 μM、4.58 μM、12.30 μM和1.650 μM。此外，Fasudil mesylate 还作为Ca2+通道拮抗剂和血管扩张剂，表现出良好的药效。

CMPD101 hydrochloride 是一种小分子抑制剂,对GRK2和GRK3表现出高度选择性,其IC50值分别为18 nM和5.4 nM, 并具有良好的膜通透性.此外,该化合物还能抑制Rho相关激酶2 (ROCK-2) 和PKCα,其IC50值分别为1.4 μM 和8.1 μM.

Nocarnickelamides B (Compound 2) 是一种线性肽类ROCK1/2抑制剂，对ROCK1和ROCK2的IC50值分别为14.9 μM和21.9 μM。其通过结合于ATP结合位点发挥作用，抑制ROCK调控的细胞骨架收缩标志物（如肌球蛋白轻链的激活）。Nocarnickelamides B 在青光眼研究中具备应用潜力。

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。