BMS-P5 Chemical Properties

InChIKey

UMXWDEKCDIDCBA-TVJVWYQLNA-N

SMILES

C(C1CC1)N1C2=NC=CC=C2C=C1C1=NC2=CC(C(N3C[C@H](N)CC[C@@H]3C)=O)=CC(OC)=C2N1C.Cl |&1:21,25,r|

BMS-P5 Usage And Synthesis

Description

BMS-P5 is a Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor with pIC50 values in the range of 5-?7.5. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays appearance of symptoms and disease progression Targeting PAD4 may be beneficial for treatment of multiple myeloma.

Biological Activity

BMS-P5 is an inhibitor of the protein arginine deiminase 4 (PAD4; IC50 = 0.098 μM). It is selective for PAD4 over PAD1, -2, and -3 (IC50s = >10 μM). BMS-P5 (1 μM) inhibits citrullination of histone H3 and neutrophil extracellular trap (NET) formation induced by RPMI-8226- or MM.1S-conditioned medium in isolated human neutrophils. It delays disease onset and increases survival in a DP42 syngeneic mouse model of multiple myeloma when administered at a dose of 50 mg/kg.