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

Sibiriline 是 RIPK1 的特异性竞争性抑制剂,靶向 RIPK1 ATP 结合位点并将其锁定在非活性构象中。Sibiriline 可抑制 TNF 诱导的 RIPK1 依赖性坏死性凋亡和 RIPK1 依赖性细胞凋亡,但不能保护细胞免于 caspase 依赖性细胞凋亡。Sibiriline 可保护小鼠免于伴刀豆球蛋白 A 诱导的肝炎,具有抑制免疫依赖性肝炎的潜力。

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Sibiriline Chemical Structure

Sibiriline Chemical Structure

CAS No. : 1346526-26-8

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查看 RIP kinase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
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]
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]
分子量

210.23

Formula

C13H10N2O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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产品名称:
Sibiriline
目录号:
HY-120600
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