For research use only. Not for therapeutic Use.
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1[1].
KB02-JQ1 (5-40 μM; 24 hours; HEK293T cells) treatment shows concentration-dependent degradation of endogenous BRD4 in HEK293T cells[1].
| Catalog Number | I017563 |
| CAS Number | 2384184-44-3 |
| Synonyms | N-[2-[2-[2-[[2-[[1-(2-chloroacetyl)-3,4-dihydro-2H-quinolin-6-yl]oxy]acetyl]amino]ethoxy]ethoxy]ethyl]-2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetamide |
| Molecular Formula | C38H43Cl2N7O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C38H43Cl2N7O6S/c1-23-24(2)54-38-35(23)36(26-6-8-28(40)9-7-26)43-30(37-45-44-25(3)47(37)38)20-32(48)41-12-15-51-17-18-52-16-13-42-33(49)22-53-29-10-11-31-27(19-29)5-4-14-46(31)34(50)21-39/h6-11,19,30H,4-5,12-18,20-22H2,1-3H3,(H,41,48)(H,42,49)/t30-/m0/s1 |
| InChIKey | XIYYDTXOEVAZGI-PMERELPUSA-N |
| SMILES | CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCNC(=O)COC4=CC5=C(C=C4)N(CCC5)C(=O)CCl)C6=CC=C(C=C6)Cl)C |
| Reference | [1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746. |
