cell-penetration

UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂，IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平，IC50为 25 nM。

UNC0646 是一种有效的、选择性的同源蛋白赖氨酸甲基转移酶 G9a 和 GLP 抑制剂，IC50分别为 6 和 15 nM，对 G9a GLP 的选择性比 SETD7、SUV39H2、SETD8 和 PRMT3 高。它降低 MDA-MB-231 细胞中H3K9me2的水平，IC50为 26 nM。

Maleimide (2,5-Pyrroledione) 可用于制备荧光探针，主要用于硫醇分析物的特异性检测。它也可用于制备用于癌症研究的抗体-药物偶联物 (ADC)。

L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.

ATP-polyamine-biotin is a cell-permeable, efficient kinase cosubstrate with conversions and kinetics similar to those of other known ATP analogues. APB shows a cytotoxicity EC50 value of 19 ± 1 mM. ATP-polyamine-biotin is shown to promote biotin labeling

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

Caprochlorone 对正痘病毒具有抗病毒活性，可以降低被感染的小鼠肺部中流感病毒的滴度。Caprochlorone 可以抑制病毒穿透细胞，并且延迟新形成的病毒从细胞释放。

hAChE Aβ1-42-IN-1 (Compound 16) 是一种有效的 hAChE 和 Aβ1-42聚集抑制剂。hAChE Aβ1-42-IN-1 对 hepG2 细胞系显示出可接受的相对安全性，并具有良好的 BBB 渗透性和较宽的安全范围。hAChE Aβ1-42-IN-1具有研究阿尔茨海默病 (AD) 的潜力。

SHP2-IN-9 is a potent inhibitor (IC50 = 1.174 μM) specifically targeting the SHP2 protein, displaying improved penetration across the blood-brain barrier. It exhibits a remarkable 85-fold selectivity for SHP2 over SHP1. By inhibiting SHP2-mediated cell signal transduction and impairing cancer cell proliferation, SHP2-IN-9 effectively suppresses the growth of both cervix cancer tumors and glioblastoma in vivo [1].

SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) and rotenone. SNJ-1945 reduces murine retinal cell death in vitro and in vivo. SNJ-1945 has good aqueous solubility, can prevents the heart from KCl arrest-reperfusion injury associated with the impairment of total Ca(2+) handling by inhibiting the proteolysis of alpha-fodrin as a cardioplegia.

Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2 M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

KOS-1584 is a second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2 M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration, and reduced CNS exposure. In addition, epothilone KOS-1584 is a poor substrate for the P-glycoprotein (P-gp) drug efflux pump.

LAH4 TFA是一种两亲性肽抗生素，以α螺旋形式表现出显著的抗菌(antimicrobial)、核酸转染(nucleic acid transfection)及细胞穿透能力。它在传递质粒DNA方面显示出较高效能，并对细菌外膜中的阴离子脂质展现强烈亲和力。

Pegsebrenatide (NLY01) 是一种具有扩展半衰期和优良血脑屏障穿透能力的长效GLP-1R激动剂。该化合物能够抑制A1型星形胶质细胞的活化，降低多巴胺能神经元凋亡，并在帕金森病（PD）小鼠模型中改善运动功能障碍。

JDB175是一种具有口服活性的高选择性BTK抑制剂，能够有效穿透血脑屏障。在中枢神经系统淋巴瘤的小鼠模型中，JDB175显示出良好的抗肿瘤活性，并未观察到显著毒性。它能有效地抑制人淋巴瘤细胞的BTK信号通路，阻止细胞周期，促进细胞凋亡。

Emetine hydrochloride (NSC 33669)，一种从ipecac根部提取的生物碱，用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4，抑制细胞自噬，并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。

This novel compound is an orally bioavailable antagonist of P2X3 P2X2 3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2 3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2 3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1 2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

LAH4 acetate 是所设计的两性肽抗生素的α -螺旋结构，能够与DNA 络合，与细胞表面膜结合后被包裹在核内体中，随着pH 值的下降破坏核内体膜。具有强大的抗菌、核酸转染和细胞渗透活性。LAH4 acetate 具有较高的质粒DNA 传递能力。LAH4 acetate 对细菌膜外膜中的阴离子脂具有很强的亲和力。

Pepinh-MYD是一款含有MyD88TIR结构域序列和蛋白转导序列的MyD88抑制剂，具备穿透细胞膜的能力。该化合物通过阻断MyD88介导的TLR通路信号传递，从而抑制免疫反应。Pepinh-MYD在探索MyD88在病毒感染过程中的角色方面具有研究潜力。