For research use only. Not for therapeutic Use.
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].
PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].
PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].
PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC50 of 7.5 nM[1].
| Catalog Number | I044618 |
| Synonyms | 8-(3,5-difluoropyridin-2-yl)-N-[2-[2-[2-[2-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-2-oxoethoxy]ethoxy]ethoxy]ethyl]-15-methyl-4-(methylsulfonylmethyl)-14-oxo-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaene-5-carboxamide |
| Molecular Formula | C53H61F2N9O11S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C53H61F2N9O11S2/c1-30-46(76-29-60-30)32-9-7-31(8-10-32)21-59-50(68)42-19-36(65)25-64(42)52(70)47(53(2,3)4)61-43(66)27-75-16-15-74-14-13-73-12-11-56-49(67)37-20-41-38(17-33(37)28-77(6,71)72)39-26-62(5)51(69)45-44(39)34(22-57-45)24-63(41)48-40(55)18-35(54)23-58-48/h7-10,17-18,20,22-23,26,29,36,42,47,57,65H,11-16,19,21,24-25,27-28H2,1-6H3,(H,56,67)(H,59,68)(H,61,66)/t36-,42+,47-/m1/s1 |
| InChIKey | GPZQCKOJSPAJES-KFRCLFBHSA-N |
| SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)COCCOCCOCCNC(=O)C4=CC5=C(C=C4CS(=O)(=O)C)C6=CN(C(=O)C7=C6C(=CN7)CN5C8=C(C=C(C=N8)F)F)C)O |
| Reference | [1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607. |
