HIPK2-IN-1
HIPK2-IN-1 is an orally active and selective HIPK2 inhibitor with an IC50 of 0.56 μM. HIPK2-IN-1 exerts antifibrotic and anti-inflammatory activities. HIPK2-IN-1 binds to HIPK2, inhibits the downstream TGF‑β/Smad3, p53, and TNF‑α/NF‑κB signaling pathways, reduces the expression of fibrotic markers, suppresses cell proliferation and migration, and alleviates renal tubular injury and collagen deposition. HIPK2-IN-1 is used for the study of renal fibrosis associated with chronic kidney disease.
For research use only. We do not sell to patients.
- Formula: C18H20N10
- Molecular Weight:376.42
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Storage:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HIPK2 0.56 μM (IC50) |
HIPK1 19.36 μM (IC50) |
HIPK3 15.08 μM (IC50) |
Smad3 |
Collagen I |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| NRK-49F | IC50 |
2.51 μM
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Inhibition of TGF-β1-stimulated NRK-49F cell viability assessed by CCK-8 assay after 48 h of incubation.
Inhibition of TGF-β1-stimulated NRK-49F cell viability assessed by CCK-8 assay after 48 h of incubation.
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42594677 |
In Vitro
HIPK2-IN-1 (AF-2) effectively inhibits HIPK2 with an IC50 of 0.56 μM, and exhibits significantly improved selectivity for HIPK2 compared with the closely related HIPK1 (IC50 = 19.36 μM) and HIPK3 (IC50 = 15.08 μM) isoforms[1].
HIPK2-IN-1 (1-5 μM; 48 h) exhibits low cytotoxicity against NRK-49F cells, with an IC50 of 2.51 μM when cells are stimulated with 10 ng/mL TGF-β1[1].
HIPK2-IN-1 (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-1 (1-5 μM; 24 h) inhibits the profibrotic TGF-β/Smad3 and p53 signaling pathways and downregulates the expression of fibrosis-related proteins in TGF-β1-stimulated NRK-49F cells[1].
HIPK2-IN-1 (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-1 (1-2 μM; 10-14 days) effectively inhibits the colony-forming proliferative capacity of TGF-β1-stimulated NRK-49F cells[1].
HIPK2-IN-1 (2.5-5 μM; 24 h) effectively blocks the migration of TGF-β1-stimulated NRK-49F fibroblasts[1].
HIPK2-IN-1 exhibits excellent in vitro stability in human liver microsomes and shows moderate, species-dependent metabolic turnover rates in liver microsomes from rats, mice, dogs, and cynomolgus monkeys[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-1 had no significant effect on cell viability at concentrations of 1, 3, and 5 μmol/L.
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Cell Line:TGF-β1 (10 ng/mL) stimulated NRK-49F cells, HK-2 cells
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Concentration:1, 3, 5 μM
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Incubation Time:24 h
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Result:Reduces HIPK2 protein expression in a dose-dependent manner, decreases phosphorylation levels of Smad3 and p53, and reverses the TGF-β1-induced upregulation of the fibrosis markers fibronectin 1, collagen I, and α-SMA in NRK-49F cells.
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Cell Line:TGF-β1 (10 ng/mL) stimulated NRK-49F cells
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Concentration:2.5, 5 μM
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Incubation Time:24 h
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Result:Inhibits the migratory capacity of NRK-49F cells in a concentration-dependent manner.
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Cell Line:TNF-α (10 ng/mL) stimulated HK-2 cells
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Concentration:1, 3, 5 μM
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Incubation Time:24 h
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Result:Reduces p65 phosphorylation in a dose-dependent manner, demonstrating inhibition of TNF-α-induced NF-κB 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:Male C57BL/6J mice (7 weeks old) were fed with 0.2% Adenine (HY-B0152)‑containing diet[1]
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Dosage:50, 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.
50 mg/kg mitigated renal tubular injury and collagen deposition, as validated by improved histopathological lesions and reduced fibrotic area in H&E and Masson trichrome staining.
100 mg/kg yielded stronger effects with further alleviation of tubular damage and interstitial collagen accumulation.
Chemical Information
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Molecular Weight 376.42
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Formula C18H20N10
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SMILES
N#CC1=C2N=C(NC3=NC(N4CCNCC4)=NC=C3)C=C(NC5CC5)N2N=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HIPK2-IN-1 Related Classifications
HY-189140 Related Classifications
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