YTH-IN-2 is a YTH domain inhibitor of YTHDC2 with an IC50 of 16.84 μM. YTH-IN-2 can serve as a lead compound for discovering efficient, selective, and cell-active small-molecule inhibitors of YTHDC2.

YM-796 dihydroxybutanedioate is a selective muscarinic M1 receptor agonist. YM-796 dihydroxybutanedioate can improve cognitive impairment and reduce amyloid plaque deposition. YM-796 dihydroxybutanedioate can be used in the research of cognitive impairment diseases such as Alzheimer's disease.

YM 133 (IMC-XV) is a semisynthetic macrolide antibiotic with potent bactericidal activity. YM 133 shows activity against Erythromycin-, Josamycin-, and rokitamycin-resistant (MIC ≥ 100 μg/mL) strains of staphylococci, streptococci, Bacteroides spp., and Clostridium spp. YM 133 exhibits excellent activity against macrolide-resistant strains and against anaerobes. YM 133 can be used for antibacterial research.

YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D.

YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors.

Y1693 is an orally active RANKL inhibitor with a Kd of 5.03 μM for hRANKL. Y1693 inhibits the activation of the downstream c-fos/NFATc1 signaling pathway by blocking its interaction with RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation and bone resorptive activity, while downregulating the mRNA and protein expressions of TRAP, cathepsin K, c-fos and NFATc1. Y1693 shows no obvious cytotoxicity to bone marrow-derived macrophages and osteoclast precursor cells, and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research related to osteoporosis and periodontal diseases.

XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer.

XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.

XH-30 is a potent, selective, and orally active PKMYT1 inhibitor, with an IC50 of 4.1 nM. XH-30 suppresses the proliferation of P53-mutated triple-negative breast cancer (TNBC) cells by inducing G2/M phase release, DNA damage, and apoptosis. XH-30 demonstrates antitumor effects in an MDA-MB-231 mouse model. XH-30 can be used for P53-mutated TNBC research.

XAT-13 is an orally active antiallergic agent. XAT-13 binds to the active pocket of MRGPRX2, and inhibits C48/80-induced calcium influx and β-hexosaminidase release. XAT-13 can be used for the research of pseudo-allergic diseases.

Xanthine oxidase-IN-23 (Compound BPF) is an orally active, reversible, mixed-type Xanthine oxidase inhibitor with an IC50 of 3.33 μM. Xanthine oxidase-IN-23 directly binds to XOD in a reversible mixed-type manner to inhibit its catalytic activity. Xanthine oxidase-IN-23 upregulates ABCG2 and downregulates GLUT9 to promote renal urate excretion. Xanthine oxidase-IN-23 reduces serum urate levels and improves renal function in hyperuricemic mice. Xanthine oxidase-IN-23 can be used in the research of hyperuricemia.

Xanthine oxidase-IN-20 is a potent and orally active xanthine oxidase (XO) inhibitor with an IC50 of 1.7 nM. Xanthine oxidase-IN-20 exhibits outstanding serum uric acid (SUA)-lowering efficacy in both mouse and rat acute hyperuricemia models. Xanthine oxidase-IN-20 shows favorable safety profile. Xanthine oxidase-IN-20 can be used for hyperuricemia and gout research.

Xanthine oxidase-IN-19 (Compound 13i) is an orally effective inhibitor of xanthine oxidase (XO), with an IC50 of 0.2 μM. Xanthine oxidase-IN-19 can significantly reduce serum uric acid levels in acute hyperuricemia rat models. Xanthine oxidase-IN-19 can be used for the study of acute hyperuricemia.

WRN inhibitor 20 (Compound 14c) is a WRN degradation agent. WRN inhibitor 20 exhibits strong degradation activity in various cells, such as HCT-116 (DC50 = 1.7 µM), SW-48 (DC50 = 3.0 µM), and SW-480 (DC50 = 5.9 µM) cells. WRN inhibitor 20 exhibits potent anti proliferative, pro apoptotic, migration inhibiting, and DNA damage inducing effects in MSI-H cells. WRN inhibitor 20 can be used for research on cancer.

Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML).

VUF5207, an Impentamine analogue, is a partial agonist of histamine H3 receptor.

VPC285785 is an orally active SARS-CoV-2 main protease inhibitor with an IC50 of 0.8 μM and a Kd of 2.7 μM. VPC285785 functionally inhibits the viral main protease-mediated processing of viral polyprotein precursors required for viral replication. VPC285785 reduces viral loads in the liver, brain and spleen tissues of MHV-infected mice. VPC285785 is applicable to the research of coronavirus infections.

VP1 ligand-1 (Scheme 1 A 1) is a VP1 ligand. VP1 ligand-1 acts as a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC) and is used for the development and design of PROTAC-based VP1 degraders, such as Jun15702. VP1 ligand-1 is applicable to EV-D68 infection research.

VHR-IN-8 (Compound SA8) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 2.4 μM. VHR-IN-8 can be used for the research of cervical cancer.

VHR-IN-4 (Compound SA7) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 1.8 μM. VHR-IN-4 can be used for the research of cervical cancer.

VHR-IN-2 (Compound SA9) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 3.1 μM. VHR-IN-2 can be used for the research of cervical cancer.

VHL Ligand 39 is a conjugate of an E3 ligase ligand, serving as a key intermediate in the synthesis of complete PROTAC molecules.

VEGFR2/HDAC-IN-1 is a dual selective enzymatic inhibitor of VEGFR2 kinase and HDAC6 with oral activity. VEGFR2/HDAC-IN-1 has an IC50 of 19.19 nM for VEGFR2 and 0.165 μM for HDAC6. VEGFR2/HDAC-IN-1 increases α-tubulin acetylation, exerts antiproliferative effects, inhibits tumor growth, and exhibits antiangiogenic activity. VEGFR2/HDAC-IN-1 can be used for the research of colorectal carcinoma and hepatocellular carcinoma.

VA-111913 (VT-913) is a vasopressin receptor V1A antagonist (Ki = 1.74 nM). VA-111913 reduces uterine contractions and improves uterine blood flow by inhibiting vasopressin, thereby alleviating dysmenorrhea. VA-111913 can be used for research on menstrual pain.

V11294 is a phosphodiesterase 4 (PDE4) inhibitor with a Ki value of 436 nM against human lung PDE4. V11294 exhibits anti-inflammation activity.

USP1-IN-14 (compound 27) is a ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of 0.001 µM. USP1-IN-14 can be used for USP1-related cancers, autoimmune and inflammatory disorders research.

UAWJ-247 is a potent and reversible SARS-CoV-2 main protease (Mpro) inhibitor with an IC50 of 0.042 μM and a Ki of 0.035 μM. UAWJ-247 can be used for the research of covid-19.

UAB116 is a Liver X Receptor (LXR)/Retinoid X Receptor (RXR) agonist. UAB116 can decreases metastatic phenotype in hepatoblastoma by inhibiting the Wnt/β-Catenin pathway via upregulation of TRIM29. UAB116 can reduce proliferation, stemness and invasiveness of metastatic hepatoblastoma cells.

UA2239 is an antimalarial agent and acyclic nucleoside phosphonate. UA2239 disrupts the essential cGMP-dependent egress pathway by decreasing cGMP levels. UA2239 targets guanylyl cyclase α. UA2239 demonstrates rapid and irreversible inhibitory effects on Plasmodium parasites.

Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer.