t 614

Iguratimod (T614) 是一种抗风湿药，作为 COX-2 的抑制剂，IC50 为 20 μM (7.7 μg/mL)。它还抑制巨噬细胞迁移抑制因子 (MIF)，IC50值为 6.81 μM。

DSS30 是一种 P25/CDK5抑制剂。DSS30通过抑制淀粉样前体蛋白裂解酶1 (BACEl) 磷酸化，减少 β-淀粉样蛋白 (Aβ) 的分泌发挥作用。DSS30 可用于预防和治疗阿尔茨海默病等神经退行性疾病。

α-NETA 是一种高效的胆碱乙酰转移酶 (ChA) 抑制剂，也是一种 ALDH1A1 和趋化因子样受体 1 (CMKLR1) 拮抗剂,抗癌活性,抑制胆碱酯酶和乙酰胆碱酯 (AChE),剂量依赖性诱导 STZ 诱导的糖尿病小鼠体重和空腹血糖水平降低,显著降低肾损伤标志物的表达,可用于研究糖尿病肾病。

APE1-IN-1 是一种可透过血脑屏障且有效的无嘌呤/嘧啶内切酶 1 (APE1) 抑制剂，具有潜在的抗肿瘤活性，可增强烷基化剂甲基甲烷磺酸盐对癌细胞的细胞毒性。

Nortadalafil (Demethyl Tadalafil) 是 demethyl Tadalafil，是一种 PDE5 抑制剂。

CXCR4 antagonist 6（compound 46）是一种高效的小分子 CXCR4 趋化因子受体抑制剂，IC50 为 79 nM；其对 CXCL12 诱导的胞质钙离子流动具有显著抑制作用，IC50 为 0.25 nM，并能显著抑制 CXCL12/CXCR4 介导的细胞迁移。在小鼠癌转移模型中，该化合物表现出显著的治疗效果，凸显其在肿瘤生物学、转移机制研究及趋化因子信号通路研究中的价值。

SIRT5 inhibitor 4 (compound 11) 是一种剂量依赖性和选择性的SIRT5（Sirtuin5）抑制剂，对SIRT5的IC50 值为26.4 μM，并且在400 μM时对SIRT1/2/3亚型无抑制作用，具有抗癌潜力。

DHFR-IN-4 是一种高效的二氢叶酸还原酶 (DHFR) 抑制剂，具有抗肿瘤活性，抑制 EGFR 和 HER2 ，可用于研究胰腺癌。

YH239-EE 是 YH239 的乙酯，是 p53-MDM2 拮抗剂和凋亡诱导剂。

SB-334867 free base (SB334867A free base) 是一种选择性的orexin-1(OX1) 受体拮抗剂。在CHO-OX1细胞中，SB-334867以浓度依赖性的方式抑制人OX1受体介导的钙反应，与人OX1受体的结合为pKi=7.17。

Anti-inflammatory agent 9 (compound 28)Anti-inflammatory agent 9 (compound 28) is a benzimidazothiazole derivative derived from tilomisole. It exhibits a higher affinity for the COX-2 enzyme compared to COX-1, thereby demonstrating promising anti-inflammatory properties. Furthermore, it demonstrates oral bioavailability [1].

3-(3-Phenoxybenzyl)amino-β-carboline is a highly effective tubulin inhibitor, selectively degrading αβ-tubulin heterodimers. It induces cell cycle arrest and apoptosis in the G2/M phase. Additionally, 3-(3-Phenoxybenzyl)amino-β-carboline displays notable anticancer activity [1].

PGN36 (Compound 18) is a potent and highly selective antagonist of the cannabinoid CB 2 receptor (CB 2 R). It exhibits exceptional affinity for CB 2 R, with a Ki value of 0.09 μM [1].

Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α -Syn) aggregation. It has potential applications in Parkinson's disease research [1].

LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].

RBM10-8不可逆地抑制人鞘氨醇-1-磷酸裂解酶（hS1PL），同时也作为酶底物发挥作用。

TRPC3/6-IN-1 is a highly potent and selective inhibitor that specifically blocks the activity of the canonical transient receptor channels TRPC3 and TRPC6. It exhibits a significant blocking potency against the human isoforms hTRPC3 and hTRPC6, with IC50 values of 1260 nM and 500 nM, respectively. This compound, TRPC3/6-IN-1, is particularly valuable for conducting research on chronic models of heart failure [1].

BChE-IN-2 (compound 22) is a highly effective inhibitor of BChE, exhibiting a Ki value of 0.099 μM. This compound represents a promising pyrimidine and pyridine derivative for investigating Alzheimer's disease (AD). [1]

CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].

IMD-0354 (IKK2 Inhibitor V) 是一种选择性IKKβ抑制剂，能够抑制 NF-κB 活性。它能够抑制 TNF-α 诱导的 NF-κB 转录活性，IC50=1.2 μM。

FAK-IN-8 (化合物 5h) 是一种FAK 抑制剂 (IC50=5.32 μM)。FAK-IN-8 具有较好的抗增殖活性，可用于癌症的研究。

InhA-IN-4 (TU14) 是一种有效的结核分枝杆菌InhA(烯酰 ACP 还原酶) 抑制剂，具有潜在的抗癌和抗增殖活性，可用于研究结核分枝杆菌感染。

Anticancer agent 47 (compound 4j) exhibits potent anticancer properties, demonstrating antiproliferative activities and inducing apoptosis as well as cell cycle arrest at G0/G1 phase. Moreover, Anticancer agent 47 has exhibited significant in vivo antitumor activities [1].