t 96

Demethylzeylasteral (T-96), isolated from Tripterygium wilfordii, has anti-inflammatory, immunosuppressive and anti-tumor activities. It inhibits the invasion of triple-negative breast cancer by blocking the TGF-β signaling pathway, and it can significantly reduce atherosclerosis.

Anti-inflammatory agent 96 (Compound 5) is a potent anti-inflammatory compound. It effectively reduces ear edema induced by TPA and paw edema caused by CFA.

Antifungalagent 96 (Compound WZ-2) is an antifungal agent with excellent blood-brain barrier permeability and brain penetration. It inhibits the growth of C. neoformans H99 and C. albicans 0304103, with MIC values of 0.016 and 32 μg/mL, respectively.

Antibacterial Agent 96 (Compound 4k) is a potent antibacterial and antitubercular compound effective against both drug-susceptible and multidrug-resistant Mycobacterium tuberculosis (M. tuberculosis) strains. However, it exhibits toxicity to HepG2 and Vero cells [1].

Anticancer Agent 96 (Compound 4) exhibits cytotoxic activities against human cancer cells [1].

Bomedemstat (IMG-7289), an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor, shows activity in mouse myeloproliferative neoplasm (MPN) models. This compound exhibits antineoplastic effects and can be used for acute myeloid leukemia (AML) and myelofibrosis (MF) research.

MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively.

ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.

CCT241161 is an orally active pan-RAF inhibitor, with IC50 values of 3, 6, 10, 15, and 30 nM for LCK, CRAF, SRC, V600E-BRAF, and BRAF, respectively. It exhibits significant activity against BRAF and NRAS mutant melanomas and demonstrates anticancer cell proliferative effects [1].

Diethylnorspermine HCl (N1,N11-Diethylnorspermine tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively stabilizes SSAT enzyme activity.

Aβ42-IN-2, a γ-secretase modulator with an IC50 of 6.5 nM for Αβ42, can be used for Alzheimer's disease research [1].

ZW4864 (free base) is an orally active and selective β-catenin/B-Cell lymphoma 9 protein-protein interaction (β-catenin/BCL9 PPI) inhibitor, with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM [1]. ZW4864 (free base) also demonstrates good pharmacokinetic properties.

Triciferol acts as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR ( IC 50 =87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Triciferol also exhibits efficacious antiproliferative and cytotoxic activities in cancer cell models in vitro [1].

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

GX 201 is a selective NaV1.7 inhibitor, IC50 of < 3.2 nM for hNaV1.7.

SIRT1-IN-1 is a selective inhibitor of SIRT1 with an IC50 of 205 nM. SIRT1-IN-1 is an inhibitor of cytomegalovirus (CMV) with antiviral activity.

Verucopeptin is a pyranized cyclic peptide and an inhibitor of hypoxia-inducible factor 1 (HIF-1). It is an antibiotic effective against B16 melanoma, with anticancer activity, lowering the expression of HIF-1 target genes and HIF-1α protein levels. It can be used in cancer research.

AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.

PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction. It enhances the immune cells' ability to kill tumor cells and demonstrates significant antitumor activity in vivo in a CT26 mouse model.

SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM, suitable for respiratory diseases research.

JNJ-54717793 is an orally active, brain-penetrating compound that acts as a selective and high-affinity antagonist of the orexin-1 receptor (OX1R) with a plasma EC50 of 85 ng/mL. It demonstrates K_i values of 16 nM for hOX1R (human OX1R) and 700 nM for hOX2R, indicating its strong preference for hOX1R over hOX2R. JNJ-54717793 is recognized for its effectiveness in the treatment of anxiety disorders.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation (IC50 = 1 μM), without blocking basal transcription driven by the β-actin promoter. It has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].