RIPK1/RIPK3-PPI-IN-1
RIPK1/RIPK3-PPI-IN-1 is an orally active dual-target inhibitor of RIPK1/RIPK3, with a Kd value of 2.4 nM for RIPK1 and 24 nM for RIPK3. RIPK1/RIPK3-PPI-IN-1 inhibits the phosphorylation of RIPK1, RIPK3 and MLKL, thereby suppressing necroptosis. RIPK1/RIPK3-PPI-IN-1 restores body temperature, improves survival rate, and reduces IL-1β/IL-6 levels in serum and multiple organs of Mus musculus, thus alleviating TNF-α-induced systemic inflammatory response syndrome. RIPK1/RIPK3-PPI-IN-1 can be used in research related to systemic inflammatory response syndrome.
For research use only. We do not sell to patients.
- CAS No.: 2915280-95-2
- Formula: C27H20F2N6O3S
- Molecular Weight:546.55
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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RIPK1 2.4 nM (Kd) |
RIPK3 24 nM (Kd) |
IL-1β |
IL-6 |
RIPK1/RIPK3-PPI-IN-1 (Compound 10) (6.7 nM; 16 h) potently suppresses necroptosis in human HT-29 cells induced by TSZ (co-induced by TNF-α, a Smac mimetic, and the pan-caspase inhibitor z-VAD-fmk (HY-16658B)), with an EC50 of 6.7 nM[1].
RIPK1/RIPK3-PPI-IN-1 (5-20 nM; 6 h) dose-dependently inhibits TSZ-induced phosphorylation of RIPK1, RIPK3 and MLKL in human HT-29 cells[1].
RIPK1/RIPK3-PPI-IN-1 (1 μM; 16 h) provides dose-dependent protection against TCZ (TNF-α, cycloheximide, z-VAD-fmk)-induced necroptosis in human HT-29 cells, and maintains normal cell morphology during necroptosis induction at a concentration of 1 μM[1].
RIPK1/RIPK3-PPI-IN-1 (16 h) exerts a dose-dependent protective effect against TZ (TNF-α and z-VAD-fmk)-induced necroptosis in mouse L929 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human HT-29 cells (TSZ-induced necroptosis model)
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Concentration:5-20 nM
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Incubation Time:6 h (TSZ stimulation)
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Result:Completely suppressed phosphorylation of RIPK1, RIPK3, and MLKL at 20 nM after 6 hours of TSZ stimulation.
Allowed detectable phosphorylation of RIPK1, RIPK3, and MLKL at 5 and 10 nM.
Completely inhibited RIPK1 and RIPK3 phosphorylation within 6 h at 20 nM, subsequently blocking MLKL phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-8 weeks old, TNF-α-induced modeling)[1]
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Dosage:5 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:i.g.; single dose
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Result:Conferred 41.7%, 83.3%, and 91.7% survival rates respectively within 24 hours.
Restored mouse body temperature to normal levels by 3 hours at all tested doses.
Reduced serum levels of IL-1β and IL-6 in a dose-dependent manner.
Significantly decreased IL-1β and IL-6 levels in multiple mouse organs compared to the model group.
Chemical Information
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CAS No. 2915280-95-2
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Molecular Weight 546.55
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Formula C27H20F2N6O3S
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SMILES
O=C(NC1=NC2=CC=C(OC3=CC=C(C(NC(C4=NC(CC5=C(C=CC=C5)F)=NN4)=O)=C3)F)C=C2S1)C6CC6
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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)
RIPK1/RIPK3-PPI-IN-1 Related Classifications
HY-183564 Related Classifications
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