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..
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1346526-26-8
- 分子式: C13H10N2O
- 分子量:210.23
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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] |
化学情報
-
CAS 番号 1346526-26-8
-
分子量 210.23
-
分子式 C13H10N2O
-
SMILES
OC1=CC=C(C=C1)C2=CC3=CC=CN=C3N2
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)