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。

ROCK-IN-12 (compound R3) 是一种特异性的ROCK抑制剂，适用于青光眼的研究。

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 HCl hydrate is an orally effective, ATP-competitive ROCK1/ROCK2 inhibitor (Ki=220 nM/300 nM) that inhibits caspase-3 and suppresses stem cell apoptosis induced by multiple conditions. It is suitable for studying induced pluripotent stem cell (iPSC) culture.

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-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。

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。

beta-Asarone (Standard) 是 beta-Asarone 的标准品。适用于定量分析、质量控制及生化实验等相关研究。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。

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。