JP-163-16 

JP-163-16 is a RelA/p65 PROTAC degrader. JP-163-16 selectively reduces the expression of RelA/p65 in a proteasome-dependent manner in cells. JP-163-16 can induce cell apoptosis by inhibiting the NF-κB signaling pathway. JP-163-16 can be used for research on RelA/p65-dependent tumours, such as chronic lymphocytic leukaemia (CLL). (Pink: RelA/p65 Ligand (HY-174865); Blue: CRBN Ligand (HY-A0003); Black: Linker; CRBN Ligand+Linker (HY-160241))^[1].

JP-163-16 (Compound 15d) (3.16-3162 nM, 48 h) has significant cytotoxicity in MEC-1 (LC₅₀ = 0.14 μM) and primary CLL (LC₅₀ = 0.23 μM) cells^[1].
JP-163-16 (3.16-3162 nM, 48 h) relies on the expression of cereblon to exert cytotoxic effects and has a weaker inhibitory effect in RPMI-8226 cells (LC₅₀ = 0.68 μM)^[1].
JP-163-16 (0.1-5 μM, 48 h) significantly inhibits the growth and induces apoptosis of MDA-MB-231 (LC₅₀ = 2.9 μM) cells by degrading the level of RelA/p65 in a proteasome-dependent manner^[1].
JP-163-16 (48 h) is less toxic in primary B-lymphocytes (LD₅₀ = 19.1 μM) and T-lymphocytes (LD₅₀ = 36.4 μM)^[1].
JP-163-16 (0-1 μM, 24 h) selectively degrades the level of RelA/p65, with little impact on RelB and cRel in MEC-1 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

777.86

C₄₂H₄₇N₇O₈

O=C(NC1=CC=C(NC(CCCOC2=C(OC)C=C3C(N=C[C@@](CCC4)([H])N4C3=O)=C2)=O)C=C1)CCCCCNC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jin P, et al. Design, synthesis and evaluation of pyrrolobenzodiazepine (PBD)-based PROTAC conjugates for the selective degradation of the NF-κB RelA/p65 subunit. RSC Med Chem. 2025 May 8.  [Content Brief]