XRF-1021
XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). 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 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.
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- CAS No.: 2968523-32-0
- 화학식: C21H21FN8
- 분자량:404.44
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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HIPK2 0.18 μM (IC50) |
NF-κB |
XRF-1021 (3-100 μM, 48 h) inhibits the proliferation of TGF-β1-stimulated NRK-49F cells, with an IC50 value of 4.87 μM, indicating potential modulation of HIPK2-mediated pathways[1].
XRF-1021 (100 μM, 24 h) directly binds to HIPK2 and exhibits high binding stability (RMSD of approximately 0.1 Å, RMSF < 0.1 Å)[1].
XRF-1021 (2.5-80 μM, 24 h) does not significantly affect the proliferation or viability of HK-2 cells at concentrations of 2.5, 5, and 10 μM[1].
XRF-1021 (2.5-10 μM, 24 h) inhibits HIPK2 and downstream signaling to attenuate fibrosis in HK-2 cells[1].
XRF-1021 (2.5-10 μM, 24 h) reduces the expression of HIPK2, FN and α-SMA proteins in NRK-49F cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TGF-β1-stimulated HK-2 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Reduced the expression levels of these fibrotic markers, including FN, α-SMA, and HIPK2 protein expression in HK-2 cells dose-dependently.
Exhibited the most pronounced inhibitory effect at 10 μmol/L.
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Cell Line:TGF-β1-stimulated HK-2 cells
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Concentration:0, 10 μM
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Incubation Time:24 h
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Result:Significantly attenuated the phosphorylation levels of both proteins, indicating effective suppression of the TGF-β and NF-κB pathways.
Effectively reversed these TGF-β1-induced increases, including Wnt/β-catenin pathway target genes (PAI-1, Axin2, and MMP7) and Notch pathway target genes (Hes1, Hey1, and Hey2).
XRF-1021 (25-100 mg/kg, p.o.) alleviates renal tubular injury, reduces interstitial fibrosis, and improves renal function by inhibiting HIPK2 and multiple downstream pro-fibrotic signaling pathways, including the TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch pathways in the C57BL/6J mouse adenine diet model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats[1]
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Dosage:25, 50 and 75 mg/kg
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Administration:oral administration (p.o.)
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Result:Partially ameliorated these pathological changes in a dose-dependent manner, with the 75 mg/kg dose showing greater efficacy.
Relieved renal injury and renal fibrosis and diminished the expression levels of related renal fibrosis indicators.
Suppressed the protein expression of fibrotic markers (FN, Collagen I, α-SMA, Vimentin) and HIPK2.
Inhibited HIPK2-regulated p53 pathway, TGF-β/Smad3, NF-κB, Wnt/β-catenin and Notch pathways.
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Animal Model:Male C57BL/6J mice (seven weeks)[1]
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Dosage:25, 50 and 100 mg/kg
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Administration:oral administration (p.o.)
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Result:Mitigated renal lesions and interstitial fibrosis in a dose-dependent manner, with the 100 mg/kg dose showing the most pronounced effect.
Reduced serum creatinine, blood urea nitrogen, and uric acid levels dose-dependently.
Downregulated the expression of HIPK2, collagen I, α-SMA, and vimentin in the kidneys of adenine-fed mice.
Reduced phosphorylation levels of Smad3, NF-κB and p53.
Chemical Information
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CAS No. 2968523-32-0
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분자량 404.44
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화학식 C21H21FN8
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SMILES
NC1=NC2=CC=CC=C2N1C3=NC=C(F)C(NC4=CC=C(N5CCNCC5)C=C4)=N3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XRF-1021 Related Classifications
HY-179378 Related Classifications
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