GSK3145095

• CAT Number: I019224
• CAS Number: 1622849-43-7
• Molecular Formula: C₂₀H₁₇F₂N₅O₂
• Molecular Weight: 397.38
• Purity: ≥95%
• Storage: Store at -20°C
• IUPAC Name: 5-benzyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide
• InChI: InChI=1S/C20H17F2N5O2/c21-13-9-12-6-7-15(19(28)25-17(12)14(22)10-13)23-20(29)18-24-16(26-27-18)8-11-4-2-1-3-5-11/h1-5,9-10,15H,6-8H2,(H,23,29)(H,25,28)(H,24,26,27)/t15-/m0/s1
• InChIKey: ATQAGKAMBISZQM-HNNXBMFYSA-N
• SMILES: C1CC2=C(C(=CC(=C2)F)F)NC(=O)C1NC(=O)C3=NNC(=N3)CC4=CC=CC=C4

GSK3145095（Cat No.:I019224） is a potent and orally active inhibitor of RIP1 kinase, an enzyme involved in regulating cell death and inflammation. It demonstrates an inhibitory concentration (IC50) of 6.3 nM against RIP1 kinase. By targeting RIP1 kinase, GSK3145095 exhibits potential antitumor effects by promoting cancer cell death and also possesses immunomodulatory properties by regulating inflammatory responses. This compound holds promise as a therapeutic agent for the treatment of various diseases, including cancer, where dysregulation of RIP1 kinase signaling is implicated.

Reference

[1]. Harris PA, ET AL. Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer. ACS Med Chem Lett. 2019 May 9;10(6):857-862.