HS-1371

SKU: orb1225658

Description

HS-1371 (HS1371) is a novel potent, ATP-competitive receptor-interacting protein kinase-3 (RIP3 or RIPK3 kinase) inhibitor with IC50 of 20.8 nM; binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro; inhibits S227 auto-phosphorylation of RIP3 in treated HT-29 cells, blocks necrosome complex formation, rescues cells from RIP3-dependent necroptotic cell death but not apoptotic cell death.

Key Properties

• CAS Number: 2158197-70-5
• MW: 384.483
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₄N₄O
• SMILES: CC1=CC=C(OC2=CC=NC3=CC(C4=CN(C5CCNCC5)N=C4)=CC=C23)C=C1
• Target: RIP kinase
• Solubility: DMSO : 16.67 mg/mL 43.36 mM

Bioactivity

• In Vitro:
  HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner. HS-1371 has an inhibitory effect on RIP3 kinase activity in various cell lines. HS-1371 (0.1, 1, 5, 10, 20 μM, 9 h) can block RIP3 S227 phosphorylation. HS-1371(0.1, 1, 5, 10 μM, 24 h) rescues cells from RIP3-dependent necroptotic cell death but not apoptotic cell death. Western blot analysis. Cell line: HT-29 cells. Concentration: 0.1, 1, 5, 10, 20 μM Incubation time: 9 hours. Result: Showed an inhibitory effect on S227 auto-phosphorylation of RIP3.

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

HS1371 | HS 1371

Quick Database Links

Gene Symbol

RIP kinase