rock-in-1

ROCK-IN-1 是一种高效的 ROCK 抑制剂，对 ROCK2 介导的信号传导有抑制作用，IC50 值为 1.2 nM。ROCK-IN-1 可用于研究神经系统疾病和炎症相关疾病。

Akt ROCK-IN-1 (B12) 是Akt和ROCK的双重抑制剂，IC50值分别为0.023 nM和1.47 nM。该化合物对神经母细胞瘤表现出抗肿瘤活性。

RhoA-ROCK-IN-1（Compound b19）为一种有效的RhoA ROCK抑制剂。该化合物在抑制细胞的增殖、迁移与侵袭方面表现出显著效果，同时还能促进细胞凋亡(apoptosis)。通过阻断RhoA ROCK信号通路，RhoA-ROCK-IN-1展现了其出色的抗癌能力。

ROCK-IN-10 (compound 50)，一种高效的ROCK抑制剂，其对ROCK1和ROCK2的IC50值为6 nM和4 nM，对其他激酶的选择性超过100倍。

ROCK-IN-11 (example 94) 是 ROCK1 和 ROCK2 的有效抑制剂，IC50 ≤ 5μM，在癌症研究中具有重要作用。

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。

SB-747651A dihydrochloride是一种与ATP竞争性相互作用的抑制剂，特别针对丝裂原和应激激活激酶1 (MSK1)，IC50值为11 nM。此化合物还能抑制PRK2、RSK1、p70S6K和ROCK-II等酶的活性。因其对上述激酶的抑制作用，SB-747651A dihydrochloride在炎症研究中显示出潜力。

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-IN-D1 is an effective and selective inhibitor of ROCK.

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).

beta-Asarone (Cis-Isoelemicin) 是一种石菖蒲中的主要成分，具有免疫抑制、促进安定、中枢神经系统抑制、降温等功能。它可透过血脑屏障，能够预防帕金森病。

Coptisine (Coptisin) 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。

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].

Y27632 is a selective ROCK inhibitor, which inhibits ET-1-induced increases in natriuretic peptide production, cell size, protein synthesis, and myofibrillar organization. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord.

ROCK2-IN-6 hydrochloride (Comp A)为一种选择性ROCK2抑制剂，适用于研究ROCK介导的疾病、自身免疫性病症与炎症。

ROCK-IN-6为一有效的ROCK2抑制剂，其IC50值为2.19 nM。该化合物具备用于研究青光眼及视网膜疾病的潜力。

ROCK-IN-7（compound 9）作为ROCK激酶抑制剂，主要应用于眼部疾病（包括青光眼及视网膜疾病）的研究领域。

ROCK-IN-8 (Example 4) 是ROCK抑制剂，IC50值不足100 nM，并显示出抗炎活性，适用于呼吸系统和胃肠道疾病的研究。

ROCK2-IN-6 (Comp A) 是一種选择性针对ROCK2的抑制剂，适用于研究ROCK介导的病症、自身免疫性疾病以及炎症。

ROCK-IN-9（Compound T345）为ROCK抑制剂。该化合物在HepG2细胞中表现出IC50为40.8 μM的细胞毒性。在小鼠模型中，ROCK-IN-9展现了良好的药代动力学特性，即使在低剂量下也能获得较高的体内暴露水平及口服生物利用度。

OXA-06 hydrochloride为一种ATP竞争性ROCK抑制剂，对非小细胞肺癌细胞系表现出阻断其贴壁依赖性生长及侵袭的能力。该化合物能够抑制丝切蛋白磷酸化，但不促进细胞凋亡。

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。