For research use only. Not for therapeutic Use.
JNJ-1013 is a potent and selective IRAK1 degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces Apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705)[1].
JNJ-1013 (Degrader-3; 1.5-10000 nM; 24 h) dose-dependently degrades IRAK1 protein with an DC50 value of 3 nM.[1].
JNJ-1013 (1 µM) decreased the expression of MG-132 (HY-13259) stiyumed IRAK1 in a dose-dependent manner[1].
JNJ-1013 (0.01, 0.03, 0.1, 0.3, 1 µM; 24 h) decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) and increases the expression of cleavaged PARP[1].
| Catalog Number | I041174 |
| CAS Number | 2597343-08-1 |
| Synonyms | N-[4-[4-[2-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-2-oxoethoxy]piperidin-1-yl]-2-methoxyphenyl]-6-(1H-pyrazol-5-yl)pyridine-2-carboxamide |
| Molecular Formula | C46H55N9O7S |
| Purity | ≥95% |
| InChI | InChI=1S/C46H55N9O7S/c1-27(29-10-12-30(13-11-29)41-28(2)47-26-63-41)49-44(59)38-23-32(56)24-55(38)45(60)42(46(3,4)5)52-40(57)25-62-33-17-20-54(21-18-33)31-14-15-36(39(22-31)61-6)51-43(58)37-9-7-8-34(50-37)35-16-19-48-53-35/h7-16,19,22,26-27,32-33,38,42,56H,17-18,20-21,23-25H2,1-6H3,(H,48,53)(H,49,59)(H,51,58)(H,52,57)/t27-,32+,38-,42+/m0/s1 |
| InChIKey | MHRNVFQJUUXQIG-VIFUUBRESA-N |
| SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)C(C)NC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)COC4CCN(CC4)C5=CC(=C(C=C5)NC(=O)C6=CC=CC(=N6)C7=CC=NN7)OC)O |
| Reference | [1]. Fu L, et al. Discovery of Highly Potent and Selective IRAK1 Degraders to Probe Scaffolding Functions of IRAK1 in ABC DLBCL. J Med Chem. 2021 Aug 12;64(15):10878-10889. |
