pb2

PB2, a tris(2-carboxyethyl)phosphine (TCEP) analogue, enhances the survival of retinal ganglion cells (RGCs) following axotomy in vitro. Even at nanomolar and picomolar concentrations, PB2 demonstrates pronounced efficacy in promoting RGC survival. Notably, PB2 exhibits superior permeability compared to TCEP. Serving as a potent reducing agent, PB2 provides robust neuroprotection for RGCs[1].

PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the ability to modulate protein-protein interaction between SARS-CoV-2 and human cells. Additionally, PB28 triggers caspase-independent apoptosis and possesses significant antitumor activity.

PB200，一种HDAC6抑制剂，具有1.97 nM的IC50值。该化合物能显著提升HDAC6的表达水平至正常，并有效减轻神经炎症，从而展现出卓越的抗抑郁作用。

PB28 dihydrochloride 是一种具有选择性和高效性的 sigma 2 (σ2) 受体激动剂和 σ1 受体拮抗剂，具有抗 SARS-CoV-2 活性和抗肿瘤活性，通过调节肾癌中的 PI3K-AKT-mTOR 信号通路来抑制细胞增殖和侵袭，抑制 SK-N-SH 神经母细胞瘤细胞内质网中的钙释放，可诱导非 caspase 依赖性的细胞凋亡。

Adezmapimod (SB 203580) 是一种 p38 MAPK 抑制剂 (IC50=0.3-0.5 μM)，具有选择性和 ATP 竞争性。Adezmapimod 具有自噬和线粒体自噬的激活活性。Adezmapimod 显示出比 PKB、LCK 和 GSK-3β 高 100 倍以上的选择性。

16α-Bromoepiandrosterone (BEA) 是一种与 DHEA 相关的水溶性合成甾醇，可用于研究 II 型糖尿病和非糖尿病结核感染。

PP7 是一种PB1-PB2互作抑制剂，IC50为 8.6 μM。PB1-PB2 抑制病毒聚合酶的活性，IC50为9.5 μM。它对甲型流感病毒 A 包括 (H1N1)pdm09 (EC50=1.4 μM)，A(H7N9)，A(H9N2) 亚型具有抗病毒活性。

M&B 2297 is a bioactive chemical.

M&B 2278 is a bioactive chemical.

FDU-PB-22 为新型合成大麻素，其在HLM中的代谢速度快速，具有12.4 min的半衰期。

JPB 25 is a bioactive chemical.

Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A Puerto Rico 8 34 (H1N1) and A Aichi 2 68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2]. Methyl brevifolincarboxylate exhibits significant DPPH radical scavenging activity with an IC50 value of 8.9 μM. [1]. Wu QY, et al. Chromatographic fingerprint and the simultaneous determination of five bioactive components of geranium carolinianum L. water extract by high performance liquid chromatography. Int J Mol Sci. 2011;12(12):8740-8749. [2]. Fang SH, et al. Anti-oxidant and inflammatory mediator's growth inhibitory effects of compounds isolated from Phyllanthus urinaria. J Ethnopharmacol. 2008;116(2):333-340.

Pimodivir, also known as VX-787, JNJ-872, is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. VX-787 binds the cap-binding domain of the PB2 subunit with a KD (dissociation constant) of 24 nM as determined by isothermal titration calorimetry (ITC). The cell-based EC50 (the concentration of compound that ensures 50% cell viability of an uninfected control) for VX-787 is 1.6 nM in a cytopathic effect (CPE) assay, with a similar EC50 in a viral RNA replication assay. VX-787 is active against a diverse panel of influenza A virus strains, including H1N1pdm09 and H5N1 strains, as well as strains with reduced susceptibility to neuraminidase inhibitors (NAIs).

7-51A为一有效PB2抑制剂，其通过ITC测定的KD值仅为1.64 nM；PB2为流感RNA依赖性RNA聚合酶（RdRP）的关键亚基。

Pimodivir is an inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. The cell-based EC50 for VX-787 is 1.6 nM in a cytopathic effect (CPE) assay. VX-787 is active against a diverse

Pimodivir (VX-787) 是一种通过口服的甲型流感病毒聚合酶抑制剂，与病毒 PB2 亚基相互作用。