For research use only. Not for therapeutic Use.
A1874（Cat No.:I019330） is a potent BRD4 degrader that belongs to the outline-based class of PROTAC-like molecules. It exhibits remarkable target protein degradation efficacy, reducing BRD4 levels by 98% at low nanomolar concentrations. A1874 functions by recruiting the E3 ligase to the BRD4 protein, leading to its ubiquitination and subsequent proteasomal degradation. This targeted degradation of BRD4 offers potential therapeutic benefits in diseases where BRD4 plays a critical role, such as cancer and inflammatory disorders. A1874 represents a promising candidate for developing novel therapies based on protein degradation strategies.
| Catalog Number | I019330 |
| CAS Number | 2064292-12-0 |
| Molecular Formula | C₅₈H₆₂Cl₃F₂N₉O₇S |
| Purity | ≥95% |
| Storage | Store at -20°C |
| IUPAC Name | (2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-N-[4-[2-[2-[2-[2-[[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]acetyl]amino]ethoxy]ethoxy]ethoxy]ethylcarbamoyl]-2-methoxyphenyl]-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-carboxamide |
| InChI | InChI=1S/C58H62Cl3F2N9O7S/c1-32-33(2)80-56-48(32)51(35-11-14-37(59)15-12-35)67-44(53-71-70-34(3)72(53)56)29-47(73)65-19-21-77-23-25-79-26-24-78-22-20-66-54(74)36-13-18-43(45(27-36)76-7)68-55(75)52-49(39-9-8-10-41(61)50(39)63)58(31-64,46(69-52)30-57(4,5)6)40-17-16-38(60)28-42(40)62/h8-18,27-28,44,46,49,52,69H,19-26,29-30H2,1-7H3,(H,65,73)(H,66,74)(H,68,75)/t44-,46-,49-,52+,58-/m0/s1 |
| InChIKey | IPNTVOAQOGRLQB-JJMBTQCASA-N |
| SMILES | CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCOCCNC(=O)C4=CC(=C(C=C4)NC(=O)C5C(C(C(N5)CC(C)(C)C)(C#N)C6=C(C=C(C=C6)Cl)F)C7=C(C(=CC=C7)Cl)F)OC)C8=CC=C(C=C8)Cl)C |
| Reference | [1]. Hines J, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262. |
