2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt TGF-beta/Smad NF-κB Apoptosis Neuronal Signaling
  3. DYRK TGF-beta/Smad NF-κB Wnt β-catenin MDM-2/p53 Notch
  4. 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.

For research use only. We do not sell to patients.

XRF-1021

XRF-1021 Chemical Structure

CAS No. : 2968523-32-0

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XRF-1021 Related Antibodies

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Description

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[1].

IC50 & Target[1]

HIPK2

0.18 μM (IC50)

NF-κB

 

In Vitro

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.

XRF-1021 Related Antibodies

Western Blot Analysis[1]

Cell Line: TGF-β1-stimulated HK-2 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: TGF-β1-stimulated HK-2 cells
Concentration: 0, 10 μM
Incubation Time: 24 h
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).
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-∞ F
Rat[1] 25 mg/kg p.o. 48.1 ng/mL 3.67 h 7.71 h 819 ng·h/mL 9.64 %
Rat[1] 5 mg/kg i.v. 884 ng/mL / 13.5 h 7704 ng·h/mL /
In Vivo

XRF-1021 (25-75 mg/kg, p.o.) inhibits HIPK2 and its downstream pathways such as TGF-β pathway, NF-κB pathway, p53 pathway, Wnt/β-catenin pathway and Notch pathway, to suppress fibrotic marker expression and alleviate renal fibrosis progression in UUO models in Sprague-Dawley (SD) rats[1].
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.

Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 25, 50 and 75 mg/kg
Administration: oral administration (p.o.)
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.
Animal Model: Male C57BL/6J mice (seven weeks)[1]
Dosage: 25, 50 and 100 mg/kg
Administration: oral administration (p.o.)
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.
Molecular Weight

404.44

Formula

C21H21FN8
CAS No.
SMILES

NC1=NC2=CC=CC=C2N1C3=NC=C(F)C(NC4=CC=C(N5CCNCC5)C=C4)=N3
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Purity & Documentation
References
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XRF-1021 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XRF-10212968523-32-0XRF1021XRF 1021DYRKTGF-beta/SmadNF-κBWntβ-cateninMDM-2/p53NotchDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseTransforming growth factor betaNuclear factor-κBNuclear factor-kappaBBeta cateninRenal fibrosisHIPK2Anti-fibrotic therapychronic kidney diseaseTGF-β1p53Wnt/β-cateninInhibitorinhibitorinhibit

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