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首页-小分子抑制剂&激动剂-Immunology/Inflammation-IRAK-UR241-2
UR241-2

Chemical Structure : UR241-2

CAS No.: 2758288-13-8

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UR241-2 (UR 241-2)

货号: PC-26786Not For Human Use, Lab Use Only.

UR241-2 is a potent and selective IRAK4 inhibitor with IC50 of 1.93 nM in HotSpot Kinase assays, inhibits NF-κβ nuclear translocation and blocks IL-1β–induced IRAK4 phosphorylation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

UR241-2 is a potent and selective IRAK4 inhibitor with IC50 of 1.93 nM in HotSpot Kinase assays, inhibits NF-κβ nuclear translocation and blocks IL-1β–induced IRAK4 phosphorylation.
UR241-2 (5 and 15 nM, 4 h) suppresses IRAK4 phosphorylation induced by hIL-1β (10 ng, 45 min) in human HCH-1 EOC cells.
UR241-2 suppresses NF-κβ activation downstream of IL-1/TLR signaling.
UR241-2 UR241-2 (20-60 uM, 48 h) resulted in a dose-dependent reduction in viability across ES2, HCH1, SKOV-3, OVCAR-3, and OVCAR-8 cell lines.
UR241-2 at 20 mg/kg (intraperitoneal, once daily) suppressed tumor growth in SKOV-3 xenograft model without overt toxicity.
UR241-2 decreases tumor burden at the needle injury site and increases the number of MHCII expressing myeloid cells in the peritoneal cavity and tumor.
UR241-2 alters ECM and neutrophil-related gene expression in tumors.

物理化学性质&存储条件

分子量 427.48
分子式 C20H21N5O4S
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

N-(4-(1,1-dioxidothiomorpholino)-2-methoxyphenyl)-6-(1H-pyrazol-3-yl)picolinamide

参考文献

1. Ho TC, et al. bioRxiv [Preprint]. 2024 Nov 11:2024.11.09.622796.

2. Ho TC, et al. Leukemia. 2026 Feb;40(2):293-303.

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