bone formation

Balicatib (AAE581) is a potent and selective inhibitor of cathepsin K, used in trials studying the treatment of osteoporosis.

Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. It indirectly decreases osteoclast differentiation by reducing the RANKL OPG ratio and directly increases osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways, thereby inducing bone formation via Runx2.

Sodium etidronate (Didronel) is a synthetic therapeutic diphosphonate analog of endogenous pyrophosphate. As a member of the family of drugs known as bisphosphonates, Sodium etidronate differs from endogenous pyrophosphate in its resistance to enzymatic hydrolysis. This agent adsorbs to hydroxyapatite cells and reduces the number of osteoclasts, thereby inhibiting abnormal bone resorption. Etidronate may also directly stimulate bone formation by osteoblasts.

XRK3F2 is an inhibitor of the p62-ZZ domain, blunts MM-induced Runx2 suppression in vitro, and induces new bone formation and remodeling in the presence of tumor in vivo.

WAY262611 is a Wnt β-catenin agonist and an inhibitor of Dkk1. It increases bone formation rate with EC50 of 0.63 μM in TCF-luciferase assay.

Eleutheroside E has anti-inflammatory effects by inhibiting NF-κB activities. Eleutheroside E significantly decreases the inflammatory cell infiltration, pannus formation, cartilage damage, bone erosion of CIA mice, the generation of TNF-α and IL-6, the m

1. Dihydrolycorine-HCL(DL) shows hypotensive effects, it can block alpha 1-adrenoceptors. 2. Dihydrolycorine is an inhibitors of protein synthesis in eukarytic cells, it halts protein synthesis in eukaryotic cells by inhibiting the peptide bone formation

1. Poncirin (Isosakuranetin-7-neohesperidoside) shows a significant in vitro inhibitory effect on the growth of the human gastric cancer cells, SGC-791, in a dose-dependent manner. 2. Poncirin prevents adipogenesis, enhances osteoblast differentiation in mesenchymal stem cellsincreased bone mineral density, and improves trabecular microarchitecture likely reflect increases bone formation and decreases bone resorption in GIO mice.

Evatanepag (CP-533536 free acid) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

Schnurri-3 inhibitor-1, a potent inhibitor of schnurri-3, is an essential regulator of bone formation in adults that can be used in osteoporosis research. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL (AC50 = 2.09 μM) [1].

GRGDSPK acetate shows inhibitory activity against integrin-fibronectin binding and can be used in research on integrins in bone formation and resorption.

CXM102 is an activator of autophagy. This compound induces autophagy in aged BMSCs, rejuvenating them and promoting their preferential differentiation into osteoblasts. CXM102 enhances the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. In middle-aged male mice, it stimulates bone anabolic metabolism, reduces marrow adipocytes, delays bone loss, lowers serum inflammation levels, reduces organ fibrosis, and extends lifespan.

Anti-osteoporosis agent-11 (compound 3k) is an anti-osteoporosis compound targeting osteoclasts. It exhibits its most prominent effect by inhibiting osteoclast differentiation, with an IC50 value of 0.36 μM. Additionally, Anti-osteoporosis agent-11 suppresses osteoclast formation, bone resorption, and the expression of osteoclast-specific genes by blocking the RANKL-induced mitogen-activated protein kinase (MAPK) and NF-κB signaling pathways.

Calcitonin-13CIC6,15NIC4(salmon) (Salmon calcitonin-13CIC6,15NIC4) TFA is a version of calcitonin(salmon) labeled with carbon-13 and nitrogen-15. This hormone regulates calcium and acts dualistically as an agonist to both amylin and calcitonin receptors, promoting bone formation while inhibiting bone resorption.

E0924G is an orally active PPARδ agonist with an EC50 of 2.82 μM. It enhances the upregulation of osteoprotegerin (OPG) expression, with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibits F-actin ring formation in RAW264.7 macrophages. Additionally, E0924G modulates bone density and bone loss in models of ovariectomy (OVX) and age-related osteoporosis.

N-Ethyl-N-nitrosourea (ENU) is a DNA alkylating agent. It induces leukemia by alkylating nucleobases, thereby damaging DNA, which leads to bone marrow suppression and the development of leukemia cells. ENU is teratogenic in vivo, causing tumor formation and foot malformations in pregnant rats. Additionally, it can result in central nervous system (CNS) tumors and genetic disorders.

SPA0355 is a thiourea derivative with antioxidant and anti-inflammatory properties. It inhibits RANKL (receptor activator of nuclear factor κB ligand)-induced osteoclastogenesis in primary bone marrow-derived macrophages and suppresses the activation of MAPKs, Akt, and NF-κB pathways. Furthermore, SPA0355 enhances osteoblast differentiation by increasing alkaline phosphatase activity and mineralized nodule formation. It protects ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it a potential candidate for studying postmenopausal osteoporosis.

CDD-1431 is a highly selective BMPR2 kinase inhibitor with a Kiapp of 20.6 nM. It inhibits BRE reporter gene activity, exhibiting an IC50 of 4.87 μM. BMPs regulate cellular processes across various tissue types such as the kidneys, skeletal muscle, heart, and reproductive organs, and can induce ectopic bone formation.

CDD-1115 is a potent and selective BMPR2 inhibitor, with an IC50 of 1.8 nM and a Kiapp of 6.2 nM. It effectively suppresses gene expression mediated by bone morphogenetic proteins (BMPs). BMPs regulate cellular processes in various tissue types, such as the kidneys, skeletal muscle, heart, and reproductive organs, and can induce ectopic bone formation.

Thonzonium bromide is a mono-cationic surfactant that is structurally similar to Farnesol as an antimicrobial agent. It inhibits proton transport in a dose-dependent manner (EC50=69 μM). It inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo.

CYM 50769 is a neuropeptide W B receptor 1 (NPBWR1, GPR7) antagonist(IC50 = 0.12 μM). CYM 50769 inhibited NPW activation of NPBWR1 with a submicromolar IC50, and displayed high selectivity against a broad array of off-targets with pharmaceutical relevance.

A 79175 is a 5-lipoxygenase inhibitor that increases bone formation.

Glucosylgalactosylhydroxylysine is a bone formation and bone resorption marker that is related to bone turnover processes during growth and development as well as metabolic bone diseases.

H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection efficiency.4 1.Park, H.S., Kim, C., and Kang, Y.K.Preferred conformations of RGDX tetrapeptides to inhibit the binding of fibrinogen to plateletsBiopolymers63(5)298-313(2002) 2.Tranqui, L., Andrieux, A., Hudry-Clergeon, G., et al.Differential structural requirements for fibrinogen binding to platelets and to endothelial cellsJ. Cell Biol.108(6)2519-2527(1989) 3.Ferris, D.M., Moodie, G.D., Dimond, P.M., et al.RGD-coated titanium implants stimulate increased bone formation in vivoBiomaterials20(23-24)2323-2331(1999) 4.Kunath, K., Merdan, T., Hegener, O., et al.Integrin targeting using RGD-PEI conjugates for in vitro gene transferJ. Gene Med.5(7)588-599(2003)