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首页-小分子抑制剂&激动剂-Others-Other Targets-E8431
E8431

Chemical Structure : E8431

CAS No.: 2419580-01-9

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E8431 (Z2371498431)

货号: PC-26242Not For Human Use, Lab Use Only.

E8431 (Z2371498431) is a specific small molecule antagonist of fusogenic protein DCSTAMP, disrupts DCSTAMP-RAP1B interaction and inhibits RAP1-RAC1 signaling-mediated cytoskeletal reorganization required for osteoclast maturation and fusion, demonstrats significant osteoclastogenesis inhibition (IC50=0.7758 μM) without cytotoxic effects on mBMMs.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

E8431 (Z2371498431) is a specific small molecule antagonist of fusogenic protein DCSTAMP, disrupts DCSTAMP-RAP1B interaction and inhibits RAP1-RAC1 signaling-mediated cytoskeletal reorganization required for osteoclast maturation and fusion, demonstrats significant osteoclastogenesis inhibition (IC50=0.7758 μM) without cytotoxic effects on mBMMs.
E8431 effectively reduces the formation of bone-resorbing cells without harming other cells.
E8431 binds to human and mouse DCSTAMP proteins with binding energies of −10.4 kcal/mol and −10.1 kcal/mol, respectively.
E8431 promotes angiogenesis in the coculture system of mEPCs with mBMMs in vitro.
potentiates osteogenic and angiogenic processes through inhibitory modulation of PDGFBB secretion from pre-osteoclastic fusion events in vitro.
E8431 directly disrupts the binding of DCSTAMP and RAP1B, effectively suppresses osteoclastogenesis by disrupting DCSTAMP-RAP1B interactions, thereby inhibiting RAP1–RAC1 signaling-mediated cytoskeletal reorganization required for osteoclast maturation and fusion.

物理化学性质&存储条件

分子量 390.48
分子式 C24H26N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Spiro[1H-indene-1,2′-morpholine]-4′-carboxamide, 2,3-dihydro-N-(6,7,8,9-tetrahydro-9-oxo-5H-benzocyclohepten-2-yl)-

参考文献

1. Zhang Z, et al. Exp Mol Med. 2025 Dec;57(12):2898-2915.

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