explants

9-Methoxycanthin-6-one has anti-tumour activity, exhibits cytotoxic activity towards KB, LU-1, LNCaP, HL-60 cancer cells and other human cancer cell lines with IC50 values around 1-4 μg/mL.

Methionylmethionine (Met-Met) significantly promotes the expression of α-s1 casein (αS1-CN) in mammary explants by enhancing the availability of intracellular substrates and activating signaling pathways mediated by JAK2-STAT5 and mTOR.

Antibacterialagent 284 (Compound 7) is an antibacterial agent with a zinc-binding structure, showing potent inhibitory activity against the Legionella pneumophila metalloprotease ProA, with an IC50 of 0.96 μM. It effectively inhibits the cleavage of type IV collagen and flagellin (ProA substrates), and reduces immune evasion within the TLR5-NF-κB pathway and neutrophil (PMN)-mediated inflammation in human lung tissue explants. Antibacterialagent 284 holds potential for Legionnaires' disease research.

CPA 926 is an orally active prodrug of Esculetin that inhibits the production of MMP in cartilage explants. It is applicable for inflammation research, including studies on experimental osteoarthritis.

ADAMTS-5-IN-4 (Compound 4b) is a selective inhibitor of ADAMTS5 with an IC₅₀ of 9.4 μM. It significantly hinders Aggrecan degradation in explant models of osteoarthritis and effectively suppresses pseudopodia extension and directional migration in ovarian cancer cells. ADAMTS-5-IN-4 also exhibits significant cytotoxicity towards HEK293T cells, human chondrocytes, and porcine cartilage explants. This compound is applicable in research related to osteoarthritis and ovarian cancer.

SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.

Quininib is a selective antagonist of CysLTR1 and CysLTR2, with IC50 values of 1.2 and 52 μM, respectively, exhibiting anti-angiogenic and anti-tumour effects.

DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants. In vivo, DPC-AJ1951 normalizes serum calcium levels in thyroidparathyroidectomized rats.

T 26c sodium is a highly potent and selective MMP13 inhibitor (IC50 = 6.9 pM). Exhibits >2600-fold selectivity for MMP13 over related MMPs. Inhibits degradation of bovine nasal septum cartilage explants in vitro . Orally bioavailable.

AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.

RO314724 is a HDAC inhibitor. RO314724 is also a a reversible, tightly binding, MMP inhibitor with a Ki of 26 nm. Matrix metalloproteinases (MMPs) belong to the key enzymes of the proteolytic destruction of cartilage matrix during chronic rheumatic diseases. Ro314724 displayed MMP-proteoglycanase inhibitory activity both in vitro and ex vivo and proved to be not harmful to the morphology, viability and proteoglycan biosynthesis of bovine articular cartilage explants.