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 is an inhibitor of αβ-tubulin that binds to the colchicine binding site, thereby hindering the dynamics of microtubule assembly.

Milademetan (DS-3032) is an orally active and potent MDM2 inhibitor with antitumor activity that induces G1 cell cycle arrest, senescence, and apoptosis.Milademetan is used in the study of acute myeloid leukemia and solid tumors.

GPR35 agonist 4 (compound 10) demonstrates high potency as a GPR35 agonist with a pEC50 of 5.86, effective on both human and rat GPR35; mutation of arginine at position 3.36 results in loss of its agonist function on GPR35 [1].

BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL).

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.