s303

Amustaline (S-303) dihydrochloride is a nucleic acid-targeted alkylator recognized for its efficacy as a pathogen inactivation agent in blood components containing red blood cells. This compound comprises three key elements: an acridine anchor (a non-covalently bonding intercalator targeting nucleic acids), an effector (a bis-alkylator group that interacts with nucleophiles), and a linker (a flexible carbon chain with a labile ester bond, hydrolyzing at neutral pH to non-reactive products).

BKS3031A 是一种抑制剂，特异性结合于 αβ-微管蛋白 (αβ-tubulin) 的秋水仙碱结合位点，抑制微管的组装动力学。

Milademetan (DS-3032) 是一种具有口服活性和有效性的 MDM2 抑制剂，具有抗肿瘤活性，诱导 G1 细胞周期阻滞、衰老和凋亡。Milademetan 可用于研究急性髓系白血病和实体肿瘤。

GPR35 agonist 4 (compound 10) 是一种有效的GPR35激动剂，其效价 pEC50为 5.86。GPR35 agonist 4 在人和大鼠 GPR35 中均显示高效价。精氨酸 3.36 的突变体可消除 GPR35 agonist 4 的激动剂功能。

BMS-303141是高效性和可渗透细胞的 ACL 抑制剂(IC50:0.13 μM)。

Milademetan is a potent and selective MDM2 inhibitor. MDM2 inhibitor DS-3032b binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53 upon oral administration. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.

SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.

TAS-303 is a selective norepinephrine reuptake inhibitor which displays significant norepinephrine transporter (NET) inhibitory activity toward serotonin or dopamine transporters. Radioligand-binding studies showed that TAS-303 selectively and potently inhibited [3H]norepinephrine binding to the human NET.