PX-12

IV-2; 2-[(1-Methylpropyl)dithio]-1H-imidazole

PX-12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme. High levels of Trx-1 have been associated with colorectal, gastric and lung cancers. PX-12 stimulates apoptosis, down-regulates HIF-1?, vascular endothelial growth factor (VEGF) and iNOS, and consequently inhibits proliferation and tumor growth in animal models. It has also been reported to inhibit tubulin polymerization in vitro, induce cell cycle arrest at G2/M phase and inhibit growth, migration and invasion of several cancer cell lines. PX-12 shows antiviral activity against HIV-1, by inhibiting the enzymatic activity of Trx1 and the Trx1-dependent disulfide reduction of gp120. Microtubule polymerization and formation of acetylated microtubules are inhibited as well, activities shown to be required for HIV-1 life cycle propagation. PX-12 has broad spectrum antimicrobial activity targeting the thioredoxin system of bacterial, fungal, protozoan and helminth pathogens without significant toxicity to the host. PX-12 potentially inhibits the 33.8-kDa Main protease (Mpro)/3C-like protease of SARS-CoV-2, consequently inhibiting viral transcription and replication and possibly inhibiting spread of COVID-19.

141400-58-0

C7H12N2S2

Determined by 1H-NMR.

BPBPYQWMFCTCNG-UHFFFAOYSA-N

Lyophilized

188.3

greater than or equal to 98% (HPLC)

CC(CC)SSC1=NC=CN1

Soluble in DMSO, ethanol or DMF (all 15mg/ml). Slightly soluble in water (~1mg/ml).

Soluble in DMSO, ethanol or DMF (all 15mg/ml). Slightly soluble in water (~1mg/ml).