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首页-小分子抑制剂&激动剂-Tyrosine Kinase-DYRK-XRF-1021
XRF-1021

Chemical Structure : XRF-1021

CAS No.: 2968523-32-0

XRF-1021 (XRF1021)

货号: PC-25696Not For Human Use, Lab Use Only.

XRF-1021 is a potent inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with IC50 of 0.18 uM, suppresses HIPK2 and blocks TGF-β/Smad3, NF-κB, Wnt/β-catenin, and Notch signaling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

XRF-1021 is a potent inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with IC50 of 0.18 uM, suppresses HIPK2 and blocks TGF-β/Smad3, NF-κB, Wnt/β-catenin, and Notch signaling.
XRF-1021 inhibits the proliferation of TGF-β1 (10 ng/mL)-stimulated NRK-49F cells, with an IC50 value of 4.87 μM after 48 h treatment.
XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA.
XRF-1021 significantly improves renal function in models with 0.2 % adenine diet and unilateral ureteral obstruction (UUO), reducing tubular injury and collagen deposition.

物理化学性质&存储条件

分子量 404.45
分子式 C21H21FN8
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

1-(5-Fluoro-4-((4-(piperazin-1-yl)phenyl)amino)pyrimidin-2-yl)-1H-benzo[d]imidazole-2-amine

参考文献

1. Xinlan Hu, et al. Eur J Med Chem. 2025 Nov 7;302(Pt 2):118353.

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