Bioactivity | 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]. |
Invitro | JNJ-1013 (Degrader-3; 1.5-10000 nM; 24 小时) 剂量依赖性地降解 IRAK1 蛋白,DC50 值为 3 nM[1]。JNJ-1013 (1 µM) 以剂量依赖性方式降低 MG-132 (HY-13259) 刺激 IRAK1 的表达[1]。JNJ-1013 (0.01, 0.03, 0.1, 0.3, 1 µM; 24 h) 降低 IRAK1、p-IKBα、pSTAT3(Tyr705) 的表达并增加 cleavaged PARP 的表达[1]。 Western Blot Analysis[1] Cell Line: |
Name | JNJ-1013 |
CAS | 2597343-08-1 |
Formula | C46H55N9O7S |
Molar Mass | 878.05 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
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. |