YAP/TAZ-TEAD-IN-3 is a YAP/TAZ-TEAD interaction inhibitor with an IC50 of 1.8 nM. YAP/TAZ-TEAD-IN-3 can be used as a TEAD1 ligand to construct PROTACs, such as PROTAC TEAD degrader-2.

Y502-3888 is a c-Myc inhibitor. Y502-3888 binds to the c-Myc G4 structure, inhibits c-Myc transcription, and downregulates c-Myc expression at both mRNA and protein levels. Y502-3888 inhibits the viability of myeloma cells and induces cell apoptosis. Y502-3888 can be used for the research of multiple myeloma.

Y207–5465 is a potent and highly selective PLK2 inhibitor with an IC50 value of 584.3 nM. Y207–5465 shows only limited anti-cancer activity in HT-29 and HCT-116 cells. Y207–5465 can be used in cancer research.

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.

XL541 is a potent, selective S1P1 antagonist. XL541 inhibits GDP-GTP exchange. XL541 causes frank surface hemorrhaging of tumors. XL541 collaborates with Paclitaxel to exhibit antitumor activity against breast cancer and lung cancer.

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.

Xemilofiban is an orally active glycoprotein IIb/IIIa blocking agent. Xemilofiban inhibits platelet aggregation. Xemilofiban reduces the incidence of thrombosis.

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-22 is an orally active inhibitor of xanthine oxidase (XO) (IC50: 0.0034 μM). Xanthine oxidase-IN-22 exhibits a mixed-type inhibition mode against XO. Xanthine oxidase-IN-22 reduces serum uric acid levels in mice. Xanthine oxidase-IN-22 can be used in research related to hyperuricemia and gout.

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.

XAN-5 is a mitochondrial DNA G-quadruplex (mtG4) ligand with a Kd of 3.8 μM. XAN-5 selectively binds and stabilizes mtG4 structures, disrupting mitochondrial gene transcription and DNA replication. XAN-5 triggers mitochondrial dysfunction, ROS overproduction, G0 phase arrest and caspase-dependent apoptosis. XAN-5 inhibits autophagy and induces immunogenic cell death. XAN-5 inhibits tumor growth in a mouse liver cancer model while enhancing tumor-infiltrating CD4+ and CD8+ T cells. XAN-5 targets two cancer resistance mechanisms simultaneously. XAN-5 can be used for the research of liver cancer.

WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer.

WWZ-11-098 is a selective CDK6 PROTAC degrader with DC50 of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia. (Pink: CDK6 ligand ; Blue: Cereblon E3 ligase ligand; Black: linker).

WWQ-03-012 is a selective deSUMOylating isopeptidases DESI2 inhibitor with an IC50 of 47.3 μM. WWQ-03-012 cans induce JAK2-V617F ubiquitination-proteasome degradation with no significant effect on wild-type JAK2. WWQ-03-012 can block JAK2-STAT3/5 signaling, inhibit cell proliferation and induce apoptosis. WWQ-03-012 has a synergistic effect in combination with Ruxolitinib, further enhancing its killing effect on JAK2 mutant cells. WWQ-03-012 can be used for the research of cancer, such as myeloproliferative neoplasms.

WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer.

WRN-IN-23 is a Werner Syndrome helicase enzyme (WRN) inhibitor. WRN-IN-23 inhibits the ATP-dependent helicase domain activity of WRN. WRN-IN-23 can be used for the research of cancers characterized by microsatellite instability (MSI) and/or defective DNA mismatch repair system (dMMR).

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.

WMK-2 is a 1,2,4,5-tetraoxane derivative and ferroptosis inducer with broad-spectrum anticancer activity. WMK-2 generates hydroxyl radicals and lipid ROS to induce ferroptosis in cancer cells and cancer stem cells. WMK-2 can be used for the research of cancer.

WMK-1 is a 1,2,4,5-tetraoxane derivative and ferroptosis inducer, with significantly higher cytotoxicity against cancer cells than non-cancerous cells. WMK-1 triggers ferroptosis in cancer cells and cancer stem cells. WMK-1 can be used for the research of cancer.

WIN 64338 is a non-peptide bradykinin B2 receptor antagonist. WIN 64338 can inhibit bradykinin-evoked trigeminal nerve stimulation.

WEE1/PKMYT1-IN-3 is the axial chiral M configuration of WEE1/PKMYT1-IN-1. WEE1/PKMYT1-IN-1 is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.

WEE1/PKMYT1-IN-2 is the axial chiral P configuration of WEE1/PKMYT1-IN-1. WEE1/PKMYT1-IN-1 is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.

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).

WCF-598 is a RXRγ (Kd: 234.2 nM) and AR-V7 PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer. (Pink: RXRγ Target protein ligand; Blue: Cereblon ligand ; Black: linker).

WB2838 is a non-steroidal androgen-receptor antagonist (IC50: 0.8 μM for partially purified rat prostate cytosol receptor). WB2838 exhibits anti-cancer activity against androgen-responsive breast cancer. WB2838 also shows the inhibitory activity against the growth of the ventral prostate induced by Testosterone propionate.

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