GSK3145095

SKU: orb1308246

Description

GSK3145095 is a potent, orally bioavailable RIPK1 inhibitor (IC50 = 5 nM). It has demonstrated immunomodulatory and anti-cancer activity in preclinical studies, including in vitro assays and in vivo models of pancreatic cancer and systemic inflammation.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1622849-43-7
• MW: 397.38
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₁₇F₂N₅O₂
• SMILES: Fc1cc(F)c2NC(=O)[C@H](CCc2c1)NC(=O)c1n[nH]c(Cc2ccccc2)n1
• Target: RIP kinase
• Solubility: DMSO:245 mg/mL (616.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.58 mM)

Bioactivity

• Target IC50:
  RIP1:6.3 nM (IC50)
• In Vitro:
  GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinase-dependent cellular responses. Highlighting its potential as a novel cancer therapy, the inhibitor was also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, GSK3145095, GSK-3145095, GSK 3145095, RIP kinase, RIPK, RIP1 kinase, RIP1, RIPkinase, Receptor-interacting protein kinases

Compound Identifiers

PubChem CID

118557502