Th1

TH1217, a potent and selective inhibitor of dCTPase pyrophosphatase 1 (dCTPase), demonstrates an IC50 value of 47 nM. It amplifies the cytotoxic impact of cytidine analogues on leukemia cells and exhibits potential against COVID-19 by modulating SARS-CoV-2 interactors.

TH1760 (MKB) is an inhibitor of NUDIX-type 15 (NUDT15, IC50= 25 nM). TH1760 can sensitize cells to 6-thioguanine by increasing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 can enhance the anti-leukemia effect of thiopurine.

MTH1-IN-2 is an inhibitor of MutT homolog 1 (MTH1), with anti-tumor activity.

TH1834 dihydrochloride, a specific Tip60 histone acetyltransferase inhibitor, induces apoptosis and enhances DNA damage in breast cancer (Type: BrCa).

MTH1 ligand 1 functions as a target protein ligand for MTH1, and is utilized in the synthesis of PROTACaTAG 2139.

MTH1 degrader-1 is an inhibitor of MTH1 aTAG and serves as a ligand for target proteins in PROTAC applications. It is used in the synthesis of PROTAC aTAG 4531.

TH152 is a general reversible ligand for LC3 GABARAP with a dissociation constant (KD) of 2 µM. LC3 GABARAP is a protein associated with autophagy.

MTH1 activator-1 is an MTH1 activator that enhances endogenous MTH1 activity and significantly reduces 8-oxo-dG levels in cellular DNA. It is useful for investigating the upregulation of oxidative damage repair in nucleotide pools and examining biological effects, as well as for studies aiming to delay or prevent tumorigenesis.

TH1338 is an orally active derivative of camptothecin with potential anti-cancer activity. TH1338 exhibits significant blood-brain barrier penetration and cytotoxicity, useful for cancer research.

ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 μM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 μM. ITH15004 (1 μM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA). 1.Calzaferri, F., Narros-Fernández, P., de Pascual, R., et al.Synthesis and pharmacological evaluation of novel non-nucleotide purine derivatives as P2X7 antagonists for the treatment of neuroinflammationJ. Med. Chem.64(4)2272-2290(2021)

TH1834 is a selective inhibitor of the Tip60 (KAT5) histone acetyltransferase (HAT). It effectively induces apoptosis and promotes DNA damage in breast cancer cells. Notably, TH1834 does not influence the activity of the MOF histone acetyltransferase, which is structurally related. Overall, TH1834 exhibits potent anticancer activity.

TH1085 is an enhancer of OGG1. TH1085 stimulates DNA repair and protects cells from the environmental hazard paraquat (PQ).

ITH12711, a PP2A ligand, can traverse the blood-brain barrier (BBB) and exerts neuroprotection by restoring PP2A-phosphatase activity [1].

TH1020 is a novel Inhibitor of Toll-Like Receptor 5 (TLR5) Flagellin Complex with promising activity (IC50 =0.85±0.12 μm) and specificity.

Resiniferatoxin ((+)-Resiniferatoxin) is a highly potent synthetic TRPV1 agonist that inhibits the production of Th1 cytokines and has anti-inflammatory activity, reducing serum levels of IL-12, INF-γ, IL-1β, TNF-α, NO, and PGE.

CMP-5 is a PRMT5 inhibitor with antiviral activity, inhibits PRMT5 methyltransferase activity, and can be used in the study of SARS virus infection.

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3 me2 demethylases JMJD3 KDM6B and UTX KDM6A (IC50=8.6 6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

1. Telocinobufagin (Telobufotoxin) is the major endogenous digitalis-like factor. 2. Telocinobufagin significantly decreases the bacterial burdens in the spleen and prolongs the survival time of FIST-immunized mice challenged with live S. typhimurium. 3. Telocinobufagin has immunomodulatory activity, can enhance a Th1 immune response to control intracellular infections, could be developed as a novel immunotherapeutic agent to treat cancer and other immune-mediated diseases.

Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) suppressed the differentiation of naive CD4+ T cells into Th1 in vitro. Furthermore, Ethyl Caffeate intensely blocked the transcriptional expression in interferon-γ-related signaling, including IFN-γ, T-bet, STAT1, and STAT4.

PA452 is a selective antagonist of retinoic X receptor (RXR) and suppresses the effect of Retinoic acid on Th1 Th2 development.

Trehalose 6-behenate is a vaccine adjuvant that skews the immune response towards Th1 Th17.

SM360320 (CL-087) is an effective and selective agonist of TLR7. SM360320 inhibits HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity. SM360320 can be used for research on acting as an immunological adjuv

GTS-21 (DMXB-A) is an α7 nAChR agonist. GTS-21 suppresses inflammation associated with rheumatoid arthritis by inhibiting RA Th1 cell differentiation.