YNT-3708 is an orexin receptor (OXR) agonist, with EC50 values of 14.6 nM and 277 nm for OX1R and OX2R, respectively.

YL-1-9 is an inhibitor of the degradation of p53 by MDM2 through strong binding to the key hydrophobic pockets of MDM2. YL-1-9 induces cell cycle arrest and apoptosis in breast cancer cells.

YJZ5118 is a CDK12/13 inhibitor with IC50 values of 39.5 nM and 26.4 nM against CDK12 and CDK13, respectively. By inducing DNA damage and Apoptosis, YJZ5118 effectively suppresses tumor cell proliferation and exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for research in the field of cancer.

XZ338 is a highly selective degrader targeting BCL-XL. XZ338 does not degrade BCL-2. XZ338 inhibits MOLT-4 cells with a IC50 value of 3.7 nM. XZ338 has anti-proliferative activity. XZ338 can be used for anti-cancer study.

XT17 is an anthrone compound with broad-spectrum antibacterial activity. It exerts its antibacterial effect by disrupting the cell wall and inhibiting DNA synthesis. XT17 exhibits weak hemolytic activity, low cytotoxicity against mammalian cell lines, and a low frequency of drug resistance. Meanwhile, XT17 shows in vivo efficacy in a mouse corneal infection model induced by Staphylococcus aureus or Pseudomonas aeruginosa. Further docking studies have confirmed that XT17 can form a stable complex with bacterial gyrase. XT17 can be used in the research of the anti - infection field.

Xeruborbactam isoboxil is a beta-lactamase inhibitor.

X-17 is a Vanin-1 Inhibitor with potent anti-inflammatory and antioxidant activities. X-17 repressrs the inflammatory factor expressions and myeloperoxidase activity, elevats the colonic glutathione reserve, and restors the intestinal barrier.

WQQ-345 is a BCAT1 inhibitor with an IC50 value of 10.8 mM. WQQ-345 can lead to a decrease in α-KG levels, an upregulation of H3K27me3 expression, a reduction in the expression of glycolytic enzymes (PFKP and LDHA), and impaired glycolytic activity in 67R cells. WQQ-345 shows tumor-suppressing activity in a 67R subcutaneous xenograft model.

Win 45164 is an orally active glucocorticoid receptor (Glucocorticoid Receptor) ligand with the activity of inhibiting the pituitary - adrenal axis. It can promote liver glycogen deposition and thymus involution in adrenalectomized male rats. Meanwhile, Win 45164 has anti - inflammatory effects. It can be used in the research of inflammatory and neurological diseases.

WEHI-3773 is an inhibitor of the interaction between VDAC2 and BAK or BAX. WEHI-3773 inhibits BAX-mediated Apoptosis by blocking the VDAC2-mediated recruitment of BAX to mitochondria. Conversely, WEHI-3773 promotes BAK-mediated Apoptosis by limiting the inhibitory sequestration of BAK by VDAC2. WEHI-3773 is promising for research in the field of anti-cancer .

VUF11207 (Compound 29) TFA is a CXCR7 agonist (pKi of 8.1) that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.

Viomycin sulfate hydrate is a potent antibiotic against Mycobacteria. Viomycin sulfate hydrate rapidly inhibits polypeptide chain elongation when added to purified endogenous Escherichia coli polysomes actively engaged in polypeptide synthesis.

VH 101-amide-piperidine-Pip-alkyne is an E3 Ligase Ligand-Linker Conjugates that can be used to synthesize PROTAC degrader. The linker part of VH 101-amide-piperidine-Pip-alkyne is tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate, and the VHL-type E3 ubiquitinase ligand is VH 101, acid.

Val-Ala-PAB-SN38 is a Drug-Linker Conjugates for ADC, composed of ADC linker Val-Ala-PAB and SN38, which is the active metabolite of the Topoisomerase I inhibitor irinotecan.

UP163 enhances the activity of ATPase, and activates valosin-containing protein (VCP) with an EC50 of 9.0 μM. UP163 reduces MG-132. Remdesivir is a nucleoside analogue with effective antiviral activity.

UP158 enhances the activity of ATPase, and activates valosin-containing protein (VCP) with an EC50 of 2.57 μM.

UP12 enhances the activity of ATPase, and activates valosin-containing protein (VCP) with an EC50 of 1.24 μM.

Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC).

UNC9435 (compound 44) is a dual inhibitor of TYRO3/MERTK with IC50 values of 3.7 nM and 1.1 nM, respectively. UNC9435 reduces colony formation in non-small cell lung cancer cultures

UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC50: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC50: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research.

UNC6535 is a potent and reversible SETDB1 triple Tudor domain (3TD) ligand, with an IC50 of 3.4 µM. UNC6535 occupies simultaneously both the TD2 and TD3 reader binding sites. UNC6535 weakly inhibits SETDB1 methyltransferase activity, with an IC50 of 84 µM for the full-length protein. UNC6535 lacks selectivity for the 3TD and may also interact with the SET domain.

UNC10013 is a SETDB1 allosteric modulator that forms a covalent bond with Cys385 in the 3TD domain, exhibiting negative allosteric regulatory activity. It has a kinact/KI value of 1.0 × 106 M-1*s-1. UNC10013 effectively disrupts SETDB1-mediated Akt methylation and holds potential value for research in cancer and neurodegenerative diseases.

UG-650 is a non-Gemini analog of UVB1 that combines the structural features of UVB1 and MC 1288. UG-650 can bind to the vitamin D receptor (VDR) and inhibit the proliferation of MCF-7 cells and the migration of MC3T3-E1 cells.

UBD1031 exhibits good affinity to the ubiquitin binding domain (UBD) of USP16 with a KD of 48 nM. UBD1031 inhibits the interaction between USP16 and ISG15 with an EC50 of 1.7 nM. UBD1031 can be used a chemical probe for USP16 UBD.

Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer activity. Type-I/-II Photosensitizer-1 exhibits significant phototoxicity against both A549 and 4T1 tumor cells. Type-I/-II Photosensitizer-1 shows a strong oxygen-independent antitumor effect under laser irradiation (IC50=1.50-1.76 μM).

TWH106 is an inhibitor for Cyclophilin (Cyp) that exhibits good affinity to CypA and CypB with KD of 53 nM and 139 nM. TWH106 inhibits the replication of HIV and HCV, exhibiting antiviral activity.

TTQ-SA is a near-infrared (NIR) spiro-AIEgen (aggregation-induced emission luminogen), that converts near-infrared light (NIR) into thermal energy, causing thermal damage and death of tumor cells. TTQ-SA exhibits cellular uptake and targeting ability in cancer cell MF-7. TTQ-SA silences the expression of survivin gene with combination of DNAzyme, enhances the sensitivity of tumor cells to photothermal therapy.

TS-002455 (Example 668) is an inhibitor for Lin28a-dep Z11 with an IC50 < 1 μM. TS-002455 is the enantiomer of TS-002266.

TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1. TrxR1 prodrug-1 exhibits significant antitumor efficiency in nude mice and NSCLC organoids.

TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity.