For research use only. Not for therapeutic Use.
KB02-JQ1(CAT: I017563) is a highly selective, PROTAC-based molecular glue degrader designed to target BRD4 while sparing BRD2 and BRD3. This bifunctional compound links the BET inhibitor JQ1 to the covalent E3 ligase recruiter KB02, enabling degradation through covalent modification of DCAF16. In HEK293T cells, KB02-JQ1 (5–40 μM, 24 h) induces concentration-dependent degradation of endogenous BRD4, offering improved durability and selectivity compared to traditional BET inhibitors. By harnessing a novel covalent E3 ligase engagement mechanism, KB02-JQ1 serves as a powerful chemical probe for studying BRD4-dependent transcription and epigenetic regulation in disease biology.
| 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% |
| IUPAC Name | 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 |
| 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 |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
