Sibiriline
Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis..
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- CAS No.: 1346526-26-8
- Formule: C13H10N2O
- Masse moléculaire:210.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
RIPK1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | EC50 |
1.2 μM
Compound: L7
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Cytotoxicity against human Jurkat cells assessed as cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as cell viability measured after 24 hrs by MTT assay
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[PMID: 38199165] |
| Jurkat | EC50 |
1200 nM
Compound: 48
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Anti-neprotic activity in human Jurkat cells assessed as reduction in TNF-induced necroptosis incubated for 24 hrs by MTS assay
Anti-neprotic activity in human Jurkat cells assessed as reduction in TNF-induced necroptosis incubated for 24 hrs by MTS assay
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[PMID: 31622096] |
| Jurkat | IC50 |
1200 nM
Compound: 64
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Anti-necroptic activity in TNF alpha induced necroptosis in FADD-deficient human Jurkat cells incubated for 24 hrs by MTS reduction assay
Anti-necroptic activity in TNF alpha induced necroptosis in FADD-deficient human Jurkat cells incubated for 24 hrs by MTS reduction assay
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[PMID: 36346971] |
| L929 | CC50 |
>50 μM
Compound: Sibiriline
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Cytotoxicity against mouse L929 cells by CCK-8 assay
Cytotoxicity against mouse L929 cells by CCK-8 assay
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[PMID: 36801518] |
| L929 | EC50 |
1.31 μM
Compound: Sibiriline
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Anti-necroptosis activity against TNFalpha/z-VAD-fmk-induced mouse L929 cell necroptosis model assessed as cell viability pretreated with compound for 1 hr followed by treated with TZ for 6 hrs
Anti-necroptosis activity against TNFalpha/z-VAD-fmk-induced mouse L929 cell necroptosis model assessed as cell viability pretreated with compound for 1 hr followed by treated with TZ for 6 hrs
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[PMID: 36801518] |
| Sf9 | IC50 |
1030 nM
Compound: 48
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Inhibition of human full length GST-tagged RIPK1 expressed in baculovirus in Sf9 insect cells incubated for 10 mins in presence of [gamma32-ATP] by SDS-PAGE based topcount scintillation counting method
Inhibition of human full length GST-tagged RIPK1 expressed in baculovirus in Sf9 insect cells incubated for 10 mins in presence of [gamma32-ATP] by SDS-PAGE based topcount scintillation counting method
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[PMID: 31622096] |
Chemical Information
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CAS No. 1346526-26-8
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Masse moléculaire 210.23
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Formule C13H10N2O
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SMILES
OC1=CC=C(C=C1)C2=CC3=CC=CN=C3N2
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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)
Sibiriline Related Classifications
HY-120600 Related Classifications
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