GSK251

• CAT Number: I045341
• CAS Number: 2125968-05-8
• Molecular Formula: C29H37FN6O4S
• Molecular Weight: 584.71
• Purity: ≥95%
• Synonyms: N-[2-[2-fluoro-4-[(4-propan-2-ylpiperazin-1-yl)methyl]phenyl]pyridin-4-yl]-2-methoxy-5-morpholin-4-ylpyridine-3-sulfonamide
• InChI: InChI=1S/C29H37FN6O4S/c1-21(2)35-10-8-34(9-11-35)20-22-4-5-25(26(30)16-22)27-17-23(6-7-31-27)33-41(37,38)28-18-24(19-32-29(28)39-3)36-12-14-40-15-13-36/h4-7,16-19,21H,8-15,20H2,1-3H3,(H,31,33)
• InChIKey: ODQVPYNCHSLNGV-UHFFFAOYSA-N
• SMILES: CC(C)N1CCN(CC1)CC2=CC(=C(C=C2)C3=NC=CC(=C3)NS(=O)(=O)C4=C(N=CC(=C4)N5CCOCC5)OC)F

GSK251 (Cat No.: I045341) is a highly potent, selective, and orally bioavailable small‑molecule inhibitor of PI3Kδ (phosphoinositide 3-kinase delta), developed by GSK. It features a novel binding mode that enhances selectivity and oral pharmacokinetics, making it one of the most promising compounds in its class. GSK251 is active in preclinical cancer models, particularly targeting PI3Kδ‑driven signaling, and is being used as a bioresearch tool to dissect PI3K/Akt/mTOR pathway biology in immuno-oncology and hematologic malignancies

Reference

[1]. Down K, et al. Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode. J Med Chem. 2021 Sep 23;64(18):13780-13792.
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