HL-8

• CAT Number: I043719
• CAS Number: 2766352-64-9
• Molecular Formula: C57H59F2N11O9S2
• Molecular Weight: 1144.27
• Purity: ≥95%
• Synonyms: (2R,4S)-1-[(2S)-2-[7-[[2-[5-[6-[5-[(2,4-difluorophenyl)sulfonylamino]-6-methoxypyridin-3-yl]imidazo[1,2-a]pyridin-3-yl]-1,3,4-oxadiazol-2-yl]benzoyl]amino]heptanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
• InChI: InChI=1S/C57H59F2N11O9S2/c1-33-49(80-32-64-33)35-17-15-34(16-18-35)27-62-52(74)44-26-39(71)31-70(44)56(75)50(57(2,3)4)65-48(72)14-8-6-7-11-23-60-51(73)40-12-9-10-13-41(40)53-66-67-55(79-53)45-29-61-47-22-19-36(30-69(45)47)37-24-43(54(78-5)63-28-37)68-81(76,77)46-21-20-38(58)25-42(46)59/h9-10,12-13,15-22,24-25,28-30,32,39,44,50,68,71H,6-8,11,14,23,26-27,31H2,1-5H3,(H,60,73)(H,62,74)(H,65,72)/t39-,44+,50+/m0/s1
• InChIKey: ACMMTSCGBPIHNT-RMNSFAHDSA-N
• SMILES: CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCCCCCNC(=O)C4=CC=CC=C4C5=NN=C(O5)C6=CN=C7N6C=C(C=C7)C8=CC(=C(N=C8)OC)NS(=O)(=O)C9=C(C=C(C=C9)F)F)O

HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases[1].

Reference

[1]. Wang H, et al. Design, synthesis and activity study of a novel PI3K degradation by hijacking VHL E3 ubiquitin ligase. Bioorg Med Chem. 2022 May 1;61:116707.
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