HIPK2-IN-2
HIPK2-IN-2 is an orally active and selective HIPK2 inhibitor with an IC50 of 0.36 μM against HIPK2. HIPK2-IN-2 reduces HIPK2 protein expression levels. HIPK2-IN-2 inhibits the proliferation and migration of renal interstitial fibroblasts, alleviates renal tubular injury and collagen deposition, and suppresses TGF-β/Smad3-mediated profibrotic signaling pathways as well as TNF-α/NF-κB-mediated inflammatory signaling pathways in renal cells. HIPK2-IN-2 is used for the study of chronic kidney disease-associated renal fibrosis.
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- 화학식: C18H20N10
- 분자량:376.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
HIPK2 0.36 μM (IC50) |
HIPK1 18.41 μM (IC50) |
HIPK3 23.32 μM (IC50) |
Collagen I |
Smad3 |
In Vitro
HIPK2-IN-2 (1-5 μM; 48 h) exhibits low cytotoxicity against NRK-49F cells, with an IC50 of 2.28 μM when cells are stimulated with 10 ng/mL TGF-β1[1].
HIPK2-IN-2 (5 μM; 24 h) directly binds to endogenous HIPK2 protein in TGF-β1-stimulated NRK-49F cells and HK-2 human proximal tubular epithelial cells, and this effect is confirmed by the increased thermal stability of HIPK2 following compound exposure[1].
HIPK2-IN-2 (1-5 μM; 24 h) inhibits TGF-β/Smad3-mediated profibrotic signaling and reduces the expression of fibrotic markers in TGF-β1-stimulated human HK-2 renal tubular epithelial cells; it also blocks the NF-κB inflammatory signaling pathway[1].
HIPK2-IN-2 (1-2 μM; 10-14 days) effectively inhibits the colony-forming proliferation capacity of TGF-β1-stimulated NRK-49F cells[1].
HIPK2-IN-2 (2.5-5 μM; 24 h) effectively blocks the migration of TGF-β1-stimulated NRK-49F fibroblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NRK‑49F cells, HK‑2 cells
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Concentration:0, 1.5, 3, 5, 15, 50 μM
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Incubation Time:24 h
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Result:Showed that HIPK2-IN-2 had no significant
effect on cell viability at concentrations of 1, 3, and 5 μmol/L.
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Cell Line:NRK‑49F cells
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Concentration:2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Inhibited migration ability of NRK‑49F cells under TGF‑β1 stimulation.
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Cell Line:NRK‑49F cells, HK‑2 cells
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Concentration:1 μM, 3 μM, 5 μM
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Incubation Time:24 h
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Result:Down‑regulated HIPK2 protein expression, suppressed TGF‑β/Smad3 signaling and decreased expression of profibrotic markers (fibronectin, collagen I, α‑SMA) under TGF‑β1 stimulation.
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Cell Line:HK‑2 cells
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Concentration:1 μM, 3 μM, 5 μM
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Incubation Time:24 h
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Result:Reduced p65 phosphorylation to block TNF‑α‑induced NF‑κB pathway activation.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (7 weeks old) were fed with 0.2% Adenine (HY-B0152)‑containing diet[1]
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Dosage:50 mg/kg, 100 mg/kg
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Administration:Oral gavage; once daily; for 4 weeks
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Result:Produced dose‑dependent renal‑protective and anti‑fibrotic effects versus adenine‑model controls.
Alleviated renal tubular injury and collagen deposition at 50 mg/kg, as validated by improved histopathological lesions and reduced fibrotic area in H&E and Masson trichrome staining.
Yielded stronger effects with further alleviation of tubular damage and renal interstitial collagen accumulation at 100 mg/kg.
- Fibrosis/Collagen Morphometry
- RNA extraction experimental
- Western Blot
- Collagen: Sirius Red Staining
- Cell migration
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Research Protocol for Inflammation-related Diseases
- Protocol For Protein Expression And Purification
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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분자량 376.42
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화학식 C18H20N10
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SMILES
N#CC1=C2N(N=C1)C(NC3CC3)=CC(NC4=NC=CC(N5CCNCC5)=N4)=N2
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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)
HIPK2-IN-2 Related Classifications
HY-189141 Related Classifications
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Keywords
- HIPK2-IN-2
- DYRK
- TGF-beta/Smad
- MDM-2/p53
- Collagen
- Dual specificity tyrosine phosphorylation regulated kinase
- Dual specificity tyrosine regulated kinase
- Transforming growth factor beta
- homeodomain-interacting protein kinase 2
- profibrotic signaling
- HIPK1
- TNF-α/NF-κB
- HIPK3
- renal interstitial fibroblasts
- renal tubular injury
- chronic kidney disease-associated renal fibrosis
- TGF-β/Smad3
- collagen deposition
- Inhibitor
- inhibitor
- inhibit