Chemical Structure : XRF-1021
CAS No.:
2968523-32-0
XRF-1021
(XRF1021)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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404.45
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Formula
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C21H21FN8
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(5-Fluoro-4-((4-(piperazin-1-yl)phenyl)amino)pyrimidin-2-yl)-1H-benzo[d]imidazole-2-amine
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References
1. Xinlan Hu, et al. Eur J Med Chem. 2025 Nov 7;302(Pt 2):118353.
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