2. Apoptosis
  3. Necroptosis RIP kinase Apoptosis
  4. 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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Sibiriline

Sibiriline Chemical Structure

CAS No. : 1346526-26-8

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Sibiriline Related Antibodies

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Description

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.[1].

IC50 & Target

RIPK1[1]
Cellular Effect
Cell Line Type Value Description References
Jurkat EC50
1.2 μM
Compound: L7
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
[PMID: 38199165]
Jurkat EC50
1200 nM
Compound: 48
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
[PMID: 31622096]
Jurkat IC50
1200 nM
Compound: 64
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
[PMID: 36346971]
L929 CC50
> 50 μM
Compound: Sibiriline
Cytotoxicity against mouse L929 cells by CCK-8 assay
Cytotoxicity against mouse L929 cells by CCK-8 assay
[PMID: 36801518]
L929 EC50
1.31 μM
Compound: Sibiriline
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
[PMID: 36801518]
Sf9 IC50
1030 nM
Compound: 48
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
[PMID: 31622096]
Molecular Weight

210.23

Formula

C13H10N2O
CAS No.
SMILES

OC1=CC=C(C=C1)C2=CC3=CC=CN=C3N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Sibiriline Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sibiriline1346526-26-8NecroptosisRIP kinaseApoptosisReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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