RIPK3-IN-8
RIPK3-IN-8 is an orally active and selective RIPK3 inhibitor with a Kd of 150 nM. RIPK3-IN-8 disrupts the formation of the RIPK3-MLKL necrosome and reduces the phosphorylation of downstream MLKL. RIPK3-IN-8 inhibits necroptosis. RIPK3-IN-8 increases the survival rate in a mouse model of TNF-α/Z-VAD-fmk (HY-16658B)-induced systemic inflammatory response syndrome. RIPK3-IN-8 is used for the research of systemic inflammatory response syndrome.
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- Formule: C18H13N3O2S
- Masse moléculaire:335.38
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Stockage:
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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Activité biologique
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Activité biologique
Description
IC50 & Target
[1]|
RIPK3 150 nM (Kd) |
IL-6 |
In Vitro
RIPK3-IN-8 (compound 20) (0.039063‑20 μM; 5-24 h) inhibits necroptosis in HT‑29 and U937 cells, with an anti-necroptosis EC50 of 0.598 μM[1].
RIPK3-IN-8 exhibits weak inhibitory activity against EGFR in HCC-827 cells (IC50 = 9500 nM); it also displays good selectivity for a panel of 80 kinases, with a Kd value of 150 nM for binding to RIPK3, and its binding interaction depends on the key amino acid residues Met98 and Asp161 [1].
RIPK3-IN-8 (0.3125‑20 μM; 2‑6 h) inhibits RIPK3 activation, reduces MLKL phosphorylation levels, and disrupts RIPK3-MLKL necrosome assembly in HT-29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:0.3125, 1.25, 5, 20 μM
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Incubation Time:5 h
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Result:Reduced the phosphorylation level of RIPK3 and MLKL induced by TSZ stimulation in a dose‑dependent manner; exerted no obvious influence on total RIPK3 and MLKL protein expression.
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Cell Line:HT-29 cells
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Concentration:20 μM
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Incubation Time:0, 6 h
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Result:Suppressed the assembly of RIPK3‑MLKL necrosome complex triggered by TSZ in a time‑dependent manner.
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Cell Line:HT‑29, U937 cells
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Concentration:0.15625, 0.3125, 0.625, 1.25, 2.5, 5, 10, 20 μM (HT-29 cells)
0.039063, 0.078125, 0.15625, 0.3125, 0.625, 1.25, 2.5, 5 μM (U937 cells) -
Incubation Time:5 h (HT-29 cells)
24 h (HT-29 cells)
10 h ((U937 cells) -
Result:Rescued cell viability dose‑dependently against TSZ‑ or TCZ‑induced necroptosis.
Failed to restore cell viability under TC‑triggered cell death in HT‑29 cells; also improved cell viability dose‑dependently in TSZ‑stimulated U937 cells.
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 (Female, 6-8 weeks old, body weights 17-20 g)[1]
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Dosage:80 mg/kg; 90 mg/kg; 100 mg/kg
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Administration:oral gavage; single pretreatment dose; 1 hour before SIRS induction
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Result:Attenuated the TNF-α/z-VAD-fmk-induced reduction in body temperature over the first 11 hours post-challenge and promoted gradual recovery toward normal body temperature.
Achieved 25% survival rate at 80 mg/kg, 50% survival rate at 90 mg/kg, and 90% survival rate at 100 mg/kg.
Reduced elevated serum levels of the pro-inflammatory cytokine IL-6, as well as the tissue injury biomarkers lactate dehydrogenase (LDH), aspartate aminotransferase (AST), creatinine, and blood urea nitrogen (BUN).
Alleviated the widespread inflammatory cell infiltration, tissue disorganization, and multi-organ damage observed in the kidneys, heart, and liver of SIRS mice, preserving normal tissue architecture.
Chemical Information
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Masse moléculaire 335.38
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Formule C18H13N3O2S
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SMILES
O=C(C1=CC=C2N=CC=C(NC3=CC=C4N=CSC4=C3)C2=C1)OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RIPK3-IN-8 Related Classifications
HY-189220 Related Classifications
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