For research use only. Not for therapeutic Use.
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1].
PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].
PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells[1].
PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells[1].
| Catalog Number | I045437 |
| CAS Number | 2488851-89-2 |
| Synonyms | N’-(3-bromo-4-fluorophenyl)-4-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]ethylamino]-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide |
| Molecular Formula | C40H53BrFN9O13 |
| Purity | ≥95% |
| InChI | InChI=1S/C40H53BrFN9O13/c41-29-26-27(4-5-30(29)42)46-37(48-56)35-36(50-64-49-35)45-9-8-43-10-12-57-14-16-59-18-20-61-22-24-63-25-23-62-21-19-60-17-15-58-13-11-44-31-3-1-2-28-34(31)40(55)51(39(28)54)32-6-7-33(52)47-38(32)53/h1-5,26,32,43-44,56H,6-25H2,(H,45,50)(H,46,48)(H,47,52,53) |
| InChIKey | BVQZWOPTIZSOAW-UHFFFAOYSA-N |
| SMILES | C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NCCOCCOCCOCCOCCOCCOCCOCCNCCNC4=NON=C4C(=NC5=CC(=C(C=C5)F)Br)NO |
| Reference | [1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953. |
