RIPK1-IN-42
RIPK1-IN-42 is an orally active RIPK1 inhibitor with a Kd of 21 nM. RIPK1-IN-42 inhibits the phosphorylation of RIPK1, suppresses the phosphorylation of downstream RIPK3 and MLKL, blocks necrosome formation, and inhibits necroptosis. RIPK1-IN-42 alleviates hypothermia, suppresses the elevation of pro-inflammatory cytokine levels, and reduces organ damage. RIPK1-IN-42 can be used for the research of systemic inflammatory response syndrome.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C23H18F2N2O3
- Masse moléculaire:408.40
-
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
RIPK1 21 nM (Kd) |
RIPK3 |
RIPK1-IN-42 (Compound W-1) (0.002441-0.3125 μM; 6 h) potently inhibits necroptosis in HT-29 cells induced by TNF-α, SM-164 (HY-15989) and Z-VAD-FMK (HY-16658B) (TSZ), with an EC50 of 38.46 nM[1].
RIPK1-IN-42 (0.1-12.8 μM; 14 h) effectively inhibits TNF-α-, Cycloheximide (HY-12320)- and Z-VAD-FMK (TCZ)-induced necroptosis in HT-29 cells in vitro in a dose-dependent manner[1].
RIPK1-IN-42 (4.6875-600 nM; 10 h) effectively inhibits TSZ-induced necroptosis in U937 cells in vitro in a dose-dependent manner[1].
RIPK1-IN-42 (6.25-400 nM; 2-6 h) inhibits TSZ-induced phosphorylation of RIPK1, RIPK3 and MLKL in HT-29 cells in a time- and dose-dependent manner[1].
RIPK1-IN-42 (400 nM; 6 h) blocks TSZ-induced necrosome formation in HT-29 cells[1].
RIPK1-IN-42 (24 h) does not inhibit cycloheximide-induced apoptosis in HT-29 cells[1].
RIPK1-IN-42 exhibits low cytotoxicity in HT-29 cells, with a CC50 greater than 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HT-29 cells
-
Concentration:400 nM (time-course); 6.25, 25, 100 and 400 nM (dose-dependent)
-
Incubation Time:2, 4 and 6 h (time-course); 5 h (dose-dependent)
-
Result:Suppressed phosphorylation of RIPK1, RIPK3, and MLKL within 2 to 6 hours of TSZ treatment at 400 nM.
Inhibited phosphorylation of RIPK1, RIPK3, and MLKL in a dose-responsive manner across 6.25-400 nM after 5 hours of TSZ treatment.
-
Cell Line:HT-29 cells
-
Concentration:400 nM
-
Incubation Time:6 h
-
Result:Reduced co-immunoprecipitation of RIPK3 with RIPK1 compared to TSZ-only treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J mice (female)[1]
-
Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg
-
Administration:p.o.; single dose 1 hour pre-challenge
-
Result:Attenuated mTNF-α/Z-VAD-FMK-induced hypothermia, with body temperatures gradually restoring to normal levels over 9 hours across all tested doses.
Achieved 40% survival at 10 mg/kg, 60% survival at 20 mg/kg, and 90% survival at 30 mg/kg.
Significantly suppressed serum elevation of pro-inflammatory cytokine interleukin-6 (mIL-6) induced by TNFα challenge.
Reduced serum levels of organ damage biomarkers (lactate dehydrogenase, aspartate aminotransferase, creatinine, blood urea nitrogen) to levels closer to healthy animals.
Attenuated histologic signs of injury (inflammatory cell infiltration, tissue disorganization, cellular damage) in the heart, liver, and kidneys.
Chemical Information
-
Masse moléculaire 408.40
-
Formule C23H18F2N2O3
-
SMILES
CN1C2=C(C=CC=C2)OC[C@H](NC(C3=CC(C4=CC(F)=CC=C4F)=CC=C3)=O)C1=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
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)
RIPK1-IN-42 Related Classifications
HY-184686 Related Classifications
Powered by Bioz