For research use only. Not for therapeutic Use.
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model[1][2][3].
KTX-582 (compound I-41) degrades IRAK4 in whole blood monocyte and lymphocyte with IC50s of <0.05 μM[4].
KTX-582 inhibits IRAK4 in human whole blood LPS TNFα with an IC50 of 0.05~1 μM[4].
| Catalog Number | I042633 |
| CAS Number | 2573298-13-0 |
| Synonyms | N-[2-[4-[[3-[3-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]cyclobutyl]oxypropyl-methylamino]methyl]cyclohexyl]-6-(2-hydroxypropan-2-yl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide |
| Molecular Formula | C45H51F3N8O7 |
| Purity | ≥95% |
| InChI | InChI=1S/C45H51F3N8O7/c1-44(2,62)31-22-34-26(19-35(31)51-40(58)33-9-5-10-37(50-33)45(46,47)48)24-55(53-34)28-13-11-25(12-14-28)23-54(3)17-6-18-63-29-20-27(21-29)49-32-8-4-7-30-39(32)43(61)56(42(30)60)36-15-16-38(57)52-41(36)59/h4-5,7-10,19,22,24-25,27-29,36,49,62H,6,11-18,20-21,23H2,1-3H3,(H,51,58)(H,52,57,59) |
| InChIKey | CKFOAVDINFHZIR-UHFFFAOYSA-N |
| SMILES | CC(C)(C1=CC2=NN(C=C2C=C1NC(=O)C3=NC(=CC=C3)C(F)(F)F)C4CCC(CC4)CN(C)CCCOC5CC(C5)NC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O)O |
| Reference | [1]. Matthew Weiss. Discovery and characterization of IRAKIMiDs: degraders targeting both IRAK4 and IMiD substrates for oncology indications. Northeastern Section, ACS (NESACS). [2]. Jennifer K. Lue, MD . Targeting MYD88-Mutant DLBCL with IRAKIMiDs: A Comparison to IRAK4 Kinase Inhibition and Evaluation of Synergy with Rational Combinations. American Society of Hematology ASH Annual Meeting [3]. Vogelmann A, Robaa D, Sippl W, Jung M. Proteolysis targeting chimeras (PROTACs) for epigenetics research. Curr Opin Chem Biol. 2020 Aug;57:8-16. [4]. Nello Mainolfi, et al. Irak degraders and uses thereof. WO/2020/113233 |
