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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Interleukin Receptor-SMI-10B13
SMI-10B13

Chemical Structure : SMI-10B13

CAS No.: 2502294-68-8

SMI-10B13

货号: PC-25197Not For Human Use, Lab Use Only.

SMI-10B13 is a first-in-class, small molecule inhibitor of Oncostatin M (OSM) with Kd of 6.6 uM, strongly inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines with IC50 of 136 and 164 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SMI-10B13 is a first-in-class, small molecule inhibitor of Oncostatin M (OSM) with Kd of 6.6 uM, strongly inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines with IC50 of 136 and 164 nM, respectively.
SMI-10B13 potently inhibits multiple OSM-mediated signaling pathways.
SMI-10B13 is likely on-target and primarily due to the disruption of OSMRβ recruitment at site III, plausibly after the OSM-gp130 complex has already formed.
SMI-10B13 significantly inhibits OSM-mediated tumor growth and increase survival.
SMI-10B13 (50 mg/kg) inhibits tumor growth in ER+ breast cancer xenograft model, inhibits metastasis in vivo.
Oncostatin M (OSM) is a proinflammatory cytokine implicated in inflammatory diseases and multiple cancers, especially breast cancer.
OSM, like all other members of the IL-6 family, is a four α-helical bundle cytokine.
OSM activates its signaling pathways by interacting with two separate receptor complexes: the OSM receptor (OSMR), which consists of glycoprotein 130 (gp130) and OSMRβ, and, to a lesser degree, the LIF receptor complex consisting of gp130/LIFRβ.

物理化学性质&存储条件

分子量 368.39
分子式 C23H16N2O3
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

(E)-3-(4,5-di(1H-indol-6-yl)furan-2-yl)acrylic acid

参考文献

1. Wolf CL, et al. J Med Chem. 2025 Aug 1. doi: 10.1021/acs.jmedchem.4c03233.

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