GSK3145095

SKU: orb1220105

Description

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic. 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. (In Vitro):GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC50 = 1.6 nM), cell death as measured by LDH release (IC50 = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC50 = 0.4 nM) .

Key Properties

• CAS Number: 1622849-43-7
• MW: 397.38
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₇F₂N₅O₂
• SMILES: FC1=CC2=C(NC(=O)[C@H](CC2)NC(=O)C2=NNC(CC3=CC=CC=C3)=N2)C(F)=C1
• Target: TNF
• Solubility: DMSO:245mg/ml (616.54 Mm; Need ultrasonic)

Bioactivity

• In Vitro:
  GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC50 = 1.6 nM), cell death as measured by LDH release (IC50 = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC50 = 0.4 nM).

Storage & Handling

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

Quick Database Links

Gene Symbol

TNF