PeptideDB

JNJ-1013

CAS: 2597343-08-1 F: C46H55N9O7S W: 878.05

JNJ-1013 is a potent and selective IRAK1 degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectivel
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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.