osteoclasts

PFI-4是一种可渗透细胞的选择性BRPF1溴结构域抑制剂，IC50为 80 nM，作用于BRPF1比作用于其他溴结构域选择性强 100 多倍。

Scutellarin (Scutellarein-7-glucuronide) 是从黄芩中分离的黄酮，可抑制破骨细胞中 RANKL 介导的 MAPK 和 NF-κB 信号通路，并下调 HCC 细胞中的 STAT3 Girdin Akt 信号通路。

Amakusamine 是一种来自 Psammocinia sp. 海绵的的吲哚生物碱，抑制 RANKL 诱导的多核破骨细胞形成的分离， 抑制核因子-κB 配体受体激活剂 （RANKL） 诱导的多核破骨细胞形成。

Sodium etidronate (Didronel) 是一种内源性 pyrophosphate 的合成治疗性 diphosphonate 类似物。作为称为 bisphosphonates 盐类药物家族的一员，etidronate disodium 与内源性 pyrophosphate 的不同之处在于其对酶水解的耐受性。该药剂吸附 hydroxyapatite 细胞并减少破骨细胞的数量，从而抑制异常骨吸收。 Etidronate 还可以直接刺激成骨细胞的骨形成。

Strontium ranelate (S12911) 是抗骨质疏松的药物，能够抑制骨吸收，促进骨形成，进而促使正骨平衡。它还能够激活非骨骼细胞中的钙敏感受体 (CaSR)，进而促进肌醇 1，4，5-三磷酸的生成及丝裂原活化的蛋白激酶信号转导。

Icariside I (Lcariside I) 是一种 Icarlin 的代谢产物，具有调节骨重塑的作用，可用于研究骨质疏松。

Cyclosporin B is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection. Cyclosporin B displays antiviral properties, inhibiting the entry of hepatitis B into hepatocytes. Cyclosporin B also

Anti-osteoporosis agent-11 (compound 3k) 是一种能够靶向并抑制破骨细胞分化的抗骨质疏松化合物，其中对破骨细胞的抑制效果尤为显著，表现在其 IC50 值为 0.36 μM。此化合物还能通过阻断rankl诱导的丝裂原活化蛋白激酶 (MAPK) 和NF-κB信号通路来抑制破骨细胞的形成、骨质吸收以及破骨细胞特异性基因的表达，显示出其潜在的医疗应用价值。

Anti-osteoporosis agent-10 作为一种有效的骨质疏松抑制剂，其通过抑制破骨细胞的生成发挥作用，其IC50为0.042 μM。此外，该化合物对PPARγ亦展示了拮抗活性，具体的EC50为0.75 μM。

AubipyOMe 是一种针对抗酒石酸酸性磷酸酶 (TRAP ACP5) 的高效抑制剂。TRAP ACP5 是在活化破骨细胞和巨噬细胞中存在的一种金属酶。该化合物对 TRAP5a 的 IC50 值为1.3 μM，对 TRAP5b 的 IC50 值为1.8 μM，能显著抑制小鼠巨噬细胞和人肺组织提取物中的 TRAP 活性。

Methopterin shows the activation and bone resorption function of murine osteoclasts.

JNJ-28312141 is an orally active CSF1R inhibitor and a FLT3 inhibitor. JNJ-28312141 is a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth a

Teriparatide acetate (Forteo) 是一种 PHT 激动剂，在 HEK293 细胞中的 IC50 为 2 nM。Teriparatide acetate 是一种重组形式的甲状旁腺激素。它是一种有效的合成代谢（即骨骼生长）剂，用于治疗某些形式的骨质疏松症。间歇使用特立帕肽比破骨细胞更能激活成骨细胞，从而导致骨骼整体增加。

The compound binds and blocks farnesyl diphosphate synthase in the HMG-CoA pathway (IC50 = 460 nM for recombinant human FPPS). It causes macrophage apoptosis and inhibits prenylation and sterol biosynthesis in purified osteoclasts.

AC708 is a small molecule CSF1R inhibitor that effectively inhibits CSF1R phosphorylation mediated by CSF-1 (IC50 = 26 nM) and IL-34 (IC50 = 33 nM). It also inhibited the activity of growth factor-dependent cells cultured in CSF-1 (IC50 = 38 nM) or IL-34

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb MK cells (IC50 = 0.7 μg ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 μM.

Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and 0.317 nM alone and with RAMP1, 2, or 3, respectively. It induces cAMP accumulation in COS-7 cells transfected with CTR2 (EC50 = 0.166 nM). Salmon calcitonin inhibits bone resorption by osteoclasts in a pit formation assay using rat bone slices (ID50 = 0.003 pg mL) and lowers calcium level in vivo in a bioassay of hypocalcemia in rats (ED15 = 33.9 mg kg). Formulations containing salmon calcitonin have been used to treat hypercalcemia, bone destruction by osteoporosis, and Paget's disease.

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V. It exhibits high affinity for these enzymes, with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Moreover, Relacatib effectively inhibits endogenous cathepsin K in situ in human osteoclasts, as well as human osteoclast-mediated bone resorption, with IC 50 values of 45 nM and 70 nM, respectively. Additionally, in vitro studies demonstrate Relacatib's inhibitory effect on bone resorption in human tissue, while in vivo studies on cynomolgus monkeys further validate its efficacy in reducing bone resorption.

Alisol B 是一种具有用于骨科疾病研究潜力的化合物，通过分化破骨细胞发挥其功能。

Cantharidin imide is a PP1 2A inhibitor found in Canarthis vesicatoria. It inhibits proliferation of colorectal cancer cells, increases MCP-1, IL-6, and IL-β levels, and inhibits differentiation and resorptive activity of osteoclasts. This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.

Anti-osteoporosis agent-4 (Compound 11h) 在生物医学领域中表现为有效抑制原代破骨细胞的分化，减弱RANKL诱导的破骨细胞生成，并展示出强抑制作用，具有 IC50 值为358.29 nM。此外，该化合物还能抑制关键的 PI3K AKT 和 IκBα NF-κB 信号通路激活，表明其在防治骨质疏松症中的潜在应用价值。

1,3-Dibenzyl-5-fluorouracil 作用于阻断破骨细胞的生成。该化合物主要通过抑制核因子 κB 配体受体激活因子 (Receptor activator of NF-κB ligand, RANKL) 和巨噬细胞集落刺激因子 (Macrophage colony-stimulating factor, M-CSF) 的信号通路，从而减少破骨细胞标记物的表达。此外，1,3-Dibenzyl-5-fluorouracil 也被广泛应用于代谢性骨病的研究领域。

WAY-325371可抑制破骨细胞的形成。