Necrostatin-34

SKU: orb1218091

Description

Necrostatin-34 is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.(In Vitro):Necrostatin-34 (Nec-34) exhibits IC50 values of 667 nM and 134 nM for TNFα in FADD def-Jurkat cells and L939 cells, respectively.Necrostatin-34 (Nec-34, 10 μM) inhibits the dimerization-induced RIPK1 activation as examined by phosphorylation of Ser166 (p-S166) of RIPK1, a biomarker for RIPK1 activation.Necrostatin-34 (Nec-34) may block TNFα-induced complex II formation by inhibiting the activation of RIPK1 kinase.

Key Properties

• CAS Number: 375835-43-1
• MW: 384.48
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₆N₄O₂S₂
• SMILES: O=C(NC1=NC=CS1)CSC2=C(C#N)C(C3=CC=C(C)C=C3)CC(N2)=O
• Target: RIP kinase
• Solubility: DMSO:125 mg/mL (325.11 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  Necrostatin-34 (Nec-34) exhibits IC50 values of 667 nM and 134 nM for TNFα in FADD def-Jurkat cells and L939 cells, respectively. Necrostatin-34 (Nec-34, 10 μM) inhibits the dimerization-induced RIPK1 activation as examined by phosphorylation of Ser166 (p-S166) of RIPK1, a biomarker for RIPK1 activation. Necrostatin-34 (Nec-34) may block TNFα-induced complex II formation by inhibiting the activation of RIPK1 kinase. Western blot analysis. Cell line: RIPK1 knockout L929 cells transfected with an expressing vector encoding an inducible and dimerizable RIPK1 fused with FKBP at the C-terminus. Concentration: 10 μM. Incubation time: 30 min (and then 100 ng/mL TNFα was added for indicated periods of time). Result: Downregulated p-S166 levels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4

Quick Database Links

Gene Symbol

RIP kinase