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.

TTP-6171 is a non-covalent inhibitor of Monkeypox virus I7L protease, and it can be used for research on poxvirus infections.

TTBK1-IN-3 (Compound 18) is a potent inhibitor of TTBK1, with a biochemical IC₅₀ of 18 nM and a cellular IC₅₀ of 259 nM. TTBK1-IN-3 can be used for research on Alzheimer's disease.

TSI-13-57 is a pan-TLR inhibitor (IC50: 2.7 μM, 6.03 μM, 7.37 μM, 6.38 μM for TLR9, TLR7, TLR2, TLR4, respectively). TSI-13-57 inhibits homodimerization of the TIR domains of MyD88. TSI-13-57 reduces systemic inflammatory responses in LPS-induced mice.

TrxR-IN-9 is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.26 μM. TrxR-IN-9 disrupts cellular redox balance. TrxR-IN-9 induces S-phase cell cycle arrest, promotes apoptosis and exhibits antiproliferative activity across cancer cells. TrxR-IN-9 exerts effects via synergistic nitric oxide (NO) and reactive oxygen species (ROS) action. TrxR-IN-9 can be used for the research of breast cancer, gastric cancer, colorectal cancer, liver cancer.

Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma.

TPP@CUR is the product formed by the esterification reaction between Curcumin and (5-hydroxy-5-oxopentyl)triphenylphosphonium bromide (TPP). TPP@CUR can be used to synthesize Ser@TPP@CUR, which can then be used in studies of acute kidney injury.

Tomoxiprole (MDL 035) is a new analgesic antiinflammatory agent. Tomoxiprole selectively inhibits cyclooxygenase-2 (IC50 = 7 nM) .

TNIK-IN-10 (Compound N15) is a TNIK inhibitor with an IC50 of 0.49 nM against human TNIK. TNIK-IN-10 inhibits the enzymatic activity of TNIK, downregulates the expression of Wnt pathway target genes c-Myc and AXIN2, and reduces the protein expression of LRP5 and LRP6. TNIK-IN-10 induces apoptosis. TNIK-IN-10 exhibits anticancer activity against colorectal cancer. TNIK-IN-10 can be used in the research of colorectal cancer.

TNIK modulator-1 (example 12) is a TNIK modulator.