JNJ-1013

JNJ-1013 is a potent and selective IRAK1 PROTAC 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) (Pink: ligand for target protein (HY-138834) ; black: linker (HY-Y1760) ; Blue: E3 ligase ligand (HY-112078) ) [1].

Product Specifications

CAS Number

[2597343-08-1]

UNSPSC

12352005

Target

Apoptosis; IRAK; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/jnj-1013.html

Purity

99.80

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

COC(C=C1N(CC2)CCC2OCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)=O)=O)=C(C=C1)NC(C6=CC=CC(C7=CC=NN7)=N6)=O

Molecular Formula

C46H55N9O7S

Molecular Weight

878.05

References & Citations

[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.