rock-in-5

ROCK-IN-5（化合物I-B-37）是一种有效的蛋白激酶抑制剂，包括ROCK、ERK、GSK 和AGC。ROCK-IN-5在心脏病、增殖性疾病和神经退行性疾病研究方面具有潜力。

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。

PT-262 是一种高效的 Rho 相关蛋白激酶（ROCK）抑制剂，其 IC50 约为 5 μM。PT-262 可诱导线粒体膜电位丧失，增强 caspase-3 的激活并促进细胞凋亡，同时通过不依赖 p53 的信号通路抑制 ERK 和 CDC2 的磷酸化，破坏细胞骨架组织和细胞迁移，从而整体上发挥广泛的抗肿瘤活性，是机制性肿瘤生物学和信号转导研究中的重要工具。

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide (T0267) 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 (T0267)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 (T0267) (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.

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。