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.

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 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-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/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).

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

VUF 4904 is an impentamine analog and a neutral antagonist of the histamine H3 receptor. VUF 4904 can be used in the research of diseases related to the function of the H3 receptor, such as Alzheimer's disease.

VU6052254, a derivative of VU0467319, is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (mAChR1) positive allosteric modulator with an EC50 of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC50 > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease.

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.

VKT-17-P4-23 is a blood-brain barrier-permeable DksA inhibitor. DksA is a highly conserved transcriptional regulator in Gram-negative bacteria, with a Kd of 124 μM. Through the DksA-regulated, SPI-2-dependent survival pathway, VKT-17-P4-23 exhibits antibacterial activity against both planktonic and intracellular pathogens such as Salmonella, and also effectively combats persistent bacteria that are difficult to eliminate. VKT-17-P4-23 can be used in studies of Salmonella infection.

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-6 is a selective vaccinia H1-related (VHR) phosphatase inhibitor with an IC50 of 74 nM. VHR-IN-6 shows very weaker inhibitory activity against MKP-1 (IC50 = 0.52 μM), CD45 (IC50 = 0.50 μM), Cdc25A (IC50 = 2.8 μM), PTP1B (IC50 = 0.42 μM), and HePTP (IC50 = 0.87 μM). VHR-IN-6 inhibits the proliferation of HeLa cells. VHR-IN-6 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-3 (Compound 1) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with a Ki of 0.81 μM. VHR-IN-3 mimics the phosphate group through the sulfonic acid group and competitively binds to the catalytic active center of VHR. VHR-IN-3 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.

VEGFR-2/c-Met/EGFR-IN-1 is a VEGFR-2/c-Met/EGFR inhibitor with IC50 values of 0.014 μM, 0.072 μM, and 0.94 μM, respectively. c-Met-IN-27 inhibits neovascularization in the chick chorioallantoic membrane (CAM) assay and exhibits in vivo anti-angiogenic activity. c-Met-IN-27 can be used in angiogenesis-related research.

Valyllysine (Val-Lys) is a renoprotective peptide. Valyllysine can be found in G. chorda soluble proteins following hydrolysis by thermolysin. Valyllysine effectively ameliorates pathological renal injury.

Val-Cit-Exatecan is a peptide-linked anti-tumor payload that can be used for the synthesis of antibody-drug conjugates (ADC). Val-Cit-Exatecan consists of DNA TopI inhibitor Exatecan and a cathepsin-cleavable ADC linker (valine-citrulline). Val-Cit-Exatecan can be used in the research of colorectal cancer, gastric cancer, breast cancer, non-small cell lung cancer, ovarian cancer, head and neck cancer, pancreatic cancer, cervical cancer, and melanoma.

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-16 is a USP1 inhibitor with an USP1-UAF1 IC50 value of 0.002 μM. USP1-IN-16 can be used in the research of USP1-related malignancies.