AD4

• CAT Number: I040724
• CAS Number: 2918262-09-4
• Molecular Formula: C55H78N4O15
• Molecular Weight: 1035.23
• Purity: ≥95%
• Synonyms: 8-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-N,N-bis[2-[[(1R,5R,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]ethyl]octanamide
• IUPAC Name: 8-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-N,N-bis[2-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]ethyl]octanamide
• InChI: InChI=1S/C55H78N4O15/c1-31-16-18-38-33(3)48(67-50-54(38)36(31)22-24-52(5,69-50)71-73-54)65-29-27-58(28-30-66-49-34(4)39-19-17-32(2)37-23-25-53(6)70-51(68-49)55(37,39)74-72-53)43(61)15-10-8-7-9-11-26-56-40-14-12-13-35-44(40)47(64)59(46(35)63)41-20-21-42(60)57-45(41)62/h12-14,31-34,36-39,41,48-51,56H,7-11,15-30H2,1-6H3,(H,57,60,62)/t31-,32-,33-,34-,36?,37?,38?,39?,41?,48+,49+,50-,51-,52-,53-,54-,55-/m1/s1
• InChIKey: ZLJLKXURBBWTFW-RJHWUJBZSA-N
• SMILES: C[C@@H]1CC[C@H]2[C@H]([C@H](O[C@H]3[C@@]24[C@H]1CC[C@](O3)(OO4)C)OCCN(CCO[C@@H]5[C@@H]([C@@H]6CC[C@H]([C@H]7[C@]68[C@H](O5)O[C@@](CC7)(OO8)C)C)C)C(=O)CCCCCCCNC9=CC=CC1=C9C(=O)N(C1=O)C1CCC(=O)NC1=O)C

AD4(CAT: I040724) is a novel artemisinin-derived PROTAC (proteolysis-targeting chimera) designed to selectively degrade PCLAF, a protein implicated in tumor progression. In RS4;11 leukemia cells, AD4 demonstrates potent degradation activity with an IC₅₀ of 0.6 nM, leading to activation of the p21/Rb tumor suppressor pathway and significant anti-tumor effects. In vivo, AD4 extends survival in RS4;11-transplanted NOD/SCID mice, highlighting its therapeutic potential. By harnessing targeted protein degradation, AD4 represents a promising strategy for hematologic cancer treatment and provides a valuable tool for studying PCLAF-related oncogenic mechanisms.