Zelenirstat

Zelenirstat
Clinical data
Other names	PCLX-001
Identifiers
	IUPAC name 2,6-Dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(2-piperazin-1-ylpyridin-4-yl)benzenesulfonamide;
CAS Number	1215011-08-7;
PubChem CID	58561243;
DrugBank	DB15567;
ChemSpider	35034199;
UNII	5HY8BYC3Q6;
ChEMBL	ChEMBL3357685;
Chemical and physical data
Formula	C24H30Cl2N6O2S
Molar mass	537.50 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C(=NN1C)CC(C)C)NS(=O)(=O)C2=C(C=C(C=C2Cl)C3=CC(=NC=C3)N4CCNCC4)Cl;
	InChI InChI=1S/C24H30Cl2N6O2S/c1-15(2)11-21-23(16(3)31(4)29-21)30-35(33,34)24-19(25)12-18(13-20(24)26)17-5-6-28-22(14-17)32-9-7-27-8-10-32/h5-6,12-15,27,30H,7-11H2,1-4H3; Key:WKTSLVQYGBHNRV-UHFFFAOYSA-N;

Zelenirstat, also known as PCLX-001, is an investigational new drug that is being evaluated for the treatment of cancer and as an antiviral agent. It is a small molecule inhibitor targets both N-myristoyltransferase 1 (NMT1) and N-myristoyltransferase 2 (NMT2) proteins, which are responsible for myristoylation. Its dual mechanism of action disrupts both cell signaling and energy production in cancer cells.

Zelenirstat is a strong pan-N myristoyl transferase inhibitor, which prevents addition of myristic acid into penultimate glycine of protein with myristoylation signal, and initially has been introduced as anti-tumor drug. It has completed phase I clinical trial and is going through escalation phase. Its prototype DDD85646 as well as other NMT inhibitors such as IMP-1088 have strong antiviral activities against viruses that required myristoylated proteins to complete their life cycle, including hemorrhagic viruses, such as lassa and argentinian virus, and pox viruses, such as vaccinia and monkeypox.