aberrant

Aberrant tau degrader 2 (Compound 4-12) 是一种用于tau蛋白降解的剂，可作为靶蛋白配体用于合成PROTAC降解剂C004019。

Aberrant tau ligand 1 是异常 tau 蛋白的配体，可用于合成异常形态的 PROTAC Tau 降解剂 [QC-01-175]。

TNO155 是具有口服活性野生型SHP2的选择性变构抑制剂 (IC50= 0.011 µM)。它有研究 RTK 依赖性恶性肿瘤（尤其是晚期实体瘤）的潜力。

AZD-9574 是 SSB 位点的 PARP1 特异性抑制剂。 AZD-9574 具有抗癌活性，可用于 HRD+ 乳腺癌和晚期实体恶性肿瘤的研究。

IACS-52825是一种具有选择性和高效性的双亮氨酸拉链激酶 (DLK) 抑制剂，可在 CIPN 小鼠模型中逆转对机械异常性疼痛，可用于研究神经系统疾病。

h-NTPDase8-IN-1 是一种特异性氨磺酰苯甲酰胺类 h-NTPDases8 抑制剂（IC 50 = 0.28 ± 0.07 μM）。h-NTPDase8-IN-1 可用于研究 h -NTPDase 表达异常带来的疾病。

3-Methoxytyramine (3-O-methyl Dopamine) 是一种多巴胺 （3-羟基酪胺）的细胞代谢物，是一种神经调节剂，诱导行为效应，诱导显着的 ERK 和 CREB 磷酸化，能够在多巴胺急性耗尽的小鼠中诱导一组复杂的异常不自主运动。

Indibulin (D 24851) 是一种口服有效的微管蛋白合成抑制剂，具有抗有丝分裂和抗肿瘤活性，且神经毒性小。它降低了肌间神经张力，产生异常的纺锤体，激活有丝分裂检查点蛋白 Mad2 和 BubR1，并诱导有丝分裂停滞和细胞凋亡。

Rogaratinib (BAY1163877) 选择性抑制成纤维细胞生长因子受体。

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。

PF-07265028 是一种HPK1抑制剂，其IC50为17 nM。在进行了体内药代动力学研究后，PF-07265028在小鼠和猴子体内表现出适中的清除率、终端半衰期、分布容积及口服生物利用度。PF-07265028定位、结合并抑制Hpk1的活性，进而阻断Hpk1介导的信号传导途径，防止Hpk1介导的免疫抑制，包括阻止T细胞受体（TCR）信号的抑制、效应T细胞的抑制、破坏异常的细胞因子表达，并消除免疫抑制性肿瘤微环境（TME）。这可能激活针对肿瘤细胞的细胞毒性T淋巴细胞（CTL）介导的免疫反应。Hpk1主要在造血细胞中表达，是TCR信号和T、B细胞激活的负向调节因子。

2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 是一种酮类和氨基酸衍生物，具有多种生物功能，包括血管舒张、免疫调节和神经调节活性。2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 是烟酸的前体。2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 的异常产生与神经系统疾病相关的认知缺陷和抑郁症状有关。2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 在某些类型的癌细胞中过度表达，可能被用作评估癌症风险的生物标志物。

Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization.

BMS-984923 是可口服且具有血脑屏障透过性的 mGluR5 沉默异构调节剂，抑制β-淀粉样蛋白寡聚体诱导的异常突触信号传导，可用于研究阿尔茨海默症。

SSE15206 是一种克服多药耐药性的微管聚合抑制剂，其在 HCT116 细胞中的 GI50值为 197 nM。由于癌细胞中纺锤体形成不完整，导致 G2 M 停滞，有丝分裂异常。

cis-4-Br-2,5-F2-PCPA (S1024) 抑制 LSD1 和 LSD2，Ki 值分别为 94 nM 和 8.4 μM。癌症干细胞中 LSD1异常表达，cis-4-Br-2,5-F2-PCPA 能够通过增加 CCRF-CEM 细胞中二甲基化组蛋白 H3 的 K4 (H3K4) 水平，抑制 LSD1活性和癌细胞增殖。

LSD1 2-IN-3 是赖氨酸特异性去甲基化酶 1 (LSD1) 的选择性抑制剂，Ki 值是 11 nM，而对LSD2的 Ki 值为 7 μM。LSD1在肿瘤干细胞中异常表达，LSD1 2-IN-3 能够抑制LSD1活性和癌细胞增殖。

(S)-Cdc7-IN-18, a potent CDC7 inhibitor, effectively impedes the overactivation of MCM2, a crucial tumor cell marker, induced by huCdc7 overexpression. Consequently, it inhibits the aberrant proliferation of tumor cells. This compound, exhibits promise for cancer disease research [1].

(R)-MLT-985 (compound 11) 是一种 MALT1 蛋白酶的有效抑制剂 (IC50: 3 nM)。(R)-MLT-985 在 Jurkat 细胞中对 MALT1 依赖性 IL-2 的 IC50 值为 20 nM。(R)-MLT-985 对 ABC-DLBCL 细胞中的生长和异常 CARD11 BCL10 MALT1 复合物信号传导具有抑制作用。

NDI-034858 (TAK-279) 是一种酪氨酸激酶2(TYK2)抑制剂( Kd＜200 pM)，靶向 Tyk2的JH2结构域，可治疗IL12和IL23异常表达引起的自身免疫性疾病。

RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1 2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf MEK ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.

RO4927350 is a potent and highly selective non-ATP-competitive MEK1 2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1 2 but also MEK1 2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1 2 rather than phospho-ERK1 2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback increase in MEK phosphorylation, which has been observed with other MEK inhibitors. RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation.

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.

AMG-337 monohydrate is a highly selective small molecule MET inhibitor. Aberrant hepatocyte growth factor (HGF) MET signaling has been implicated in hepatocarcinogenesis, suggesting that MET may serve as an attractive therapeutic target in hepatocellular carcinoma.