TK-684 is a potent and selective allosteric SHP2 inhibitor with IC50 values of 2.1, ＞1000 nM for SHP2WT, SHP22PTP, respectively. TK-684 inhibits cell proliferation and induces apoptosis. TK-684 decreases the protein expression of p-AKT, p-ERK.

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.

CS47 is a reversible Thioredoxin reductase 1 (TrxR1) inhibitor. CS47 activates stress-responsive GSH and iron regulatory programs, depleting GSH and promoting HO-1 overexpression and intracellular iron overload by ROS accumulation, and finally inducing ferroptosis in KRAS-independent lung cancers. CS47 has an anticancer activity with low cytotoxicity toward normal lung fibroblasts.

F 2833 is a lipid-lowering agent. F 2833 can reduce the levels of cholesterol, triglycerides, and plasma phospholipids. F 2833 can be used for research on diseases such as hyperlipidemia.

TK-685 is an orally active, selective, and allosteric SHP2 inhibitor with an IC50 of 2.1 nM. TK-685 inhibits esophageal cancer cell proliferation and induced apoptosis by targeting SHP2-mediated AKT and ERK signaling pathways.

Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments.

HBI-2375 (HYBI-084) is a selective, brain-penetrant and orally active MLL1-WDR5 interaction inhibitor. HBI-2375 inhibits WDR5 with an IC50 of 4.48 nM. HBI-2375 shows inhibition of proliferation in MV4;11 leukemia cells (IC50: 3.17 µM). HBI-2375 is capable of targeted disruption of histone methyltransferase activity in cancer cells. HBI-2375 can be used for the study of leukemia, glioma and glioblastoma.

RWJ-68022 (Example 9) is a cyclopentene derivative and a motilin receptor antagonist. RWJ-68022 can compete with motilin and erythromycin for the motilin receptor site. RWJ-68022 can be used in the research of gastrointestinal-related diseases.

IMB-881 is an antibacterial agent. IMB-881 binds to LptA to inhibit the interaction between LptA and LptC. IMB-881 shows potent antibacterial activity against Gram-negative bacteria.

GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM).

AGU661 is a Microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with an IC50 of 0.22  nM. AGU661 lowers PGE2 formation in human pro-inflammatory M1 macrophages and activated monocytes without affecting other lipid mediator pathways. AGU661 has unfavorable physicochemical properties with poor metabolic stability and strong plasma protein binding tendencies. AGU661 into PLGA-based NPs significantly enhances its bioactivity. AGU661 can be used for inflammatory disorders research.

POI ligand-2 is a ligand for GPX4 protein. POI ligand-2 can be used to synthesize PROTAC, such as PROTAC GPX4 degrader-5.

SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist)) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.

NC-1175 (hydrochloride) is an antifungal agent targeting cell membrane H+-ATPase. NC-1175 (hydrochloride) can be used for the research of infection.

STING ligand-4 (Compound 2) is a nitro-free covalent STING inhibitor with an IC50 < 0.2 μM. STING ligand-4 can be used for synthesis of PROTAC STING degrader-4.

BCL6 ligand-4 is an BCL6 ligand that can be used in the synthesis of PROTACs, such as BCL6 PROTAC 1.

ONO-1714 is an orally active nitric oxide synthase inhibitor. ONO-1714 attenuates endotoxin-induced acute lung injury, reduces intestinal ischemia–reperfusion injury, represses biliary carcinogenesis.

SC-42867 is a PGE2 antagonist. SC-42867 can be metabolized in the liver through oxidative N-dealkylation, aromatic hydroxylation, and binding reactions. SC-42867 can be used for research on metabolic conditions.

SS-750 is an orally active Triazole derivative and antifungal agent. SS-750 binds to fungal cytochrome P450. SS-750 shows antifungal activities against Candida species and C. neoformans strains tested. SS750 shows MIC90 values of 0.25, 1, and 2 μg/mL against Candida parapsilosis, C. krusei, and C. glabrata, respectively. SS-750 improves systemic and pulmonary candidiasis caused by C. albicans.

RS-79948-197 hemihydrate is a non-imidazoline α2-adrenoceptor antagonist. RS-79948-197 hemihydrate shows Kd values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively.

MolPort-010-778-422 is a high-affinity inhibitor targeting the ACE2 receptor of SARS-CoV-2 virus. MolPort-010-778-422 demonstrates excellent antiviral activity (IC50=8.9 nM). MolPort-010-778-422 is promising for research of SARS-CoV-2.

APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research.

BAL-1516 is a brain-penetrant and highly selective NLRP3 inhibitor (IC50=14.2 nM). BAL-1516 significantly suppresses IL-1β and IL-18 release in microglial neuroinflammation models (IC50=11-59 nM). BAL-1516 is promising for research of neurodegenerative diseases (e.g., Alzheimer’s, Parkinson’s) and systemic inflammatory disorders.

NZ-107 is an orally active leukotriene receptor antagonist. NZ-107 can inhibit anaphylaxis reaction. NZ-107 can be used for the researches of inflammation and immunology.

MG-HuR2 is a molecular glue degrader targeting the oncogenic RNA-binding protein HuR (IC50=0.5 μM). MG-HuR2 is promising for research of HuR-overexpressing malignancies (e.g., breast cancer).

Di-Ellipticine-RIBOTAC TFA (Compound 7) is a RNA RIBOTAC degrader, capable of specifically binding and degrading r(G4C2)exp. Di-Ellipticine-RIBOTAC TFA only cuts the expanded GGGGCC repeat RNA in the pathogenic factor of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) - the chromosome 9 open reading frame 72 (9orf72) gene (r(G4C2)exp), and has no effect on normal short repetitive sequences. Di-Ellipticine-RIBOTAC TFA significantly improves the pathological phenotype of c9ALS/FTD in cells and mouse models. Di-Ellipticine-RIBOTAC TFA can be used for the study of c9ALS/FTD.

Wy 27569 is an orally active vascular selective calcium channel blocker that can effectively lower blood pressure. Wy 27569 is a thromboxane synthase inhibitor that can reshape prostaglandin balance, reduce pro thrombotic TXA2, and increase anti thrombotic PGI2. Wy 27569 can be used for research on cardiovascular diseases such as hypertension and angina.

TEI-2306 is a precursor of glutathione biosynthesis. TEI-2306 possesses a unique anti-HIV-1 activity in both chronically and acutely infected cells, and even for free viruses. TEI-2306 can be used for the study of myocardial ischaemia.

Emvistegrast is a quinolone derivative. Emvistegrast is an antagonist of α4β7 integrin. Emvistegrast can be studied in research for diseases that are mediated by α4β7 integrin, such as infkammatory bowel disease.

NSC 303861 is an L-glutamine antagonist. NSC 303861 selectively inhibits glutamine dependent enzymes in purine nucleotide synthesis without affecting pyrimidine synthase. NSC 303861 has significant cytotoxicity against liver cancer 3924A cells (LC50 = 6 µM). NSC 303861 can be used for cancer research.