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。

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。

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。

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。

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。

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.

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。

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].

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。