RGNCY-0111 (ETS (IMMLG-537 ) LAPTM4B-35 inhibitor)

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ETS (IMMLG-537 s a small molecule with effective anti-cancer activity by targeting LAPTM4B-35.  LAPTM4B-35 is over-expressed in a  variety of slid cancers including hepatocarcinoma cells (HCC).  This over-expression leads to carcinogenesis, enhanced cancer growth, metasatsis and multi-drug resistance.  ETS has a specific and significant lethality on human HCC cells (HepG2 and Bel-7402)by inducing apoptosis but not on cultured human fetal liver cells.  Furthermore, ETS attenuated growth and metastasis of human HCC xenograft models in nude mice and extended the lifespan of the HCC mice. The killing effect of ETS was attenuated when LAPTM4B-35 over-expression was knocked down using RNAi.  The changes in expression of c-Myc, Bcl-2, Bax, cyclinD1 and Akt-p in HepG2 cells driven by LAPTM4B-35 over-expression could be reversed by ETS.  Therefore, ETS is a promising candidate for the treatment of HCC and other sold tumors.  HepG2 IC50 = 0.9µmol/L, Bel-7402 IC50 = 0.7 µmol/L.

Systematic Name:  (2Z,2'E)-2,2'-(butane-1,2-diylidene)bis(hydrazine-1-carbothioamide)

SMILES:  NC(N/N=C/C(CC)=N\NC(N)=S)=S

Formula:  C6H12N6S2

Mol Wt:  232.32

PMID:  2742271