osteoclast

Zoledronic acid monohydrate (CGP 42446) is a synthetic imidazole bisphosphonate analog with anti-bone-resorption activity.

Usnic Acid (Usniacin) is an antimicrobial, antitumor and enzyme inhibiting agent shown to uncouple oxidative phosphorylation in mouse-liver mitochondria. Usnic acid induces necrosis in certain cells.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).

Wedelolactone (IKK Inhibitor II) is a natural product derived from Eclipta prostrata that inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα, and exhibits anticancer, anti-inflammatory, and antioxidant activities. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells by downregulating PKCε, without inhibiting Akt. Wedelolactone inhibits 5-Lox with an IC50 value of 2.5 μM. Wedelolactone can be used in research on inflammation, tumors, liver disease, and immune-related diseases.

Velutin shows the strongest inhibitory effect in NF-κB activation and exhibits the greatest effects in blocking the degradation of inhibitor of NF-κB as well as in inhibiting mitogen-activated protein kinase p38 and JNK phosphorylation. Velutin has anti-inflammatory property. Velutin exhibits the greatest potency among all flavones which reduce TNF-α and IL-6 production.

Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavone II may have therapeutic potential for the treatment of allergic asthma.Skullcapflavone II regulates osteoclast differentiation, survival, and function. Skullcapflavone II exerts potent antimicrobial activity against M. aurum and M. bovis BCG

6''-O-acetylsaikosaponin A is an acetyl saikosaponin isolated from the roots of Bupleurum chinense. Itshows some osteoclast-inhibiting activities

Methysticin is a kavalactone isolated from the kava roots. Methylsticin (Methysticin) exhibit osteoclast formation inhibitory activity. It inhibits activation of NF-χB in lung adenocarcinoma tissue, activates Nrf2 in neurons and astroglia, decreases peak amplitude of voltage-gated Na+ channels in hippocampal neurons, and suppresses growth of Fusarium, Trichoderma, and Colletotrichum.

Toddaculine may be beneficial for the prevention and treatment of osteoporosis, it can not only inhibit the differentiation of osteoclasts via activation of the NF-κB, ERK 1/2, and p38 MAPK signaling pathways, but can induce differentiation and mineralization of osteoblasts by regulating differentiation factors. Toddaculine also may serve as a pharmacological prototype for the development of novel anti-leukemic agents, it displays a dual effect as a cell differentiating agent and apoptosis inducer in U-937 cells.

VUF11207 fumarate is an agonist of CXCR7 and a high-potency ligand of CXCR7 (pKi: 8.1).

Clodronic acid disodium salt (Lodronate), a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

WAY-325398 is a furan derivatives. WAY-325398 inhibits osteoclast formation, inhibition rate is 14.11% at 10 μM.

PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.

Sciadopitysin may prevent the development of diabetic osteopathy, it exerts its therapeutic effects via upregulation of mitochondrial biogenesis.Sciadopitysin shows protective effects on antimycin A-induced toxicity in osteoblastic MC3T3-E1 cells, it may

4-IPP (4-Iodo-6-phenylpyrimidine) is an irreversible inhibitor of macrophage migration inhibitory factor (MIF).

NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.

Gossypin has antidiabetic, antioxdiant, anticonvulsant, anti-allergic, antiinflammatory, antinociceptive, cytotoxic and antibacterial activities; it inhibits the NF-kappaB activation pathway, which may explain its role in the suppression of inflammation,

Omaveloxolone (RTA-408) is an oral, potent, and selective activator of the nuclear factor erythropoietin-related factor 2 (Nrf2) pathway, as well as a low-potency PPARγ agonist. Omaveloxolone inhibits osteoclast formation by suppressing the STING-dependent NF-κB signaling pathway. Omaveloxolone is being investigated for use in ALS, multiple sclerosis, non-alcoholic steatohepatitis, neurodegenerative diseases, and oncology research.

Tiludronate disodium (Tiludronic acid disodium) is an osteoclast vacuolar H(+)-ATPase inhibitor with antiresorptive and anti-inflammatory properties. Tiludronate disodium can be used in studies about metabolic bone disorders.

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.

FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces bone metastasis of B16-F10 cells.

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1/2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.