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LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).

LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase)[1].

In summary, LCL521 acted as a specific inhibitor of the cellular ACDase, whereas the mono DMG-B13 prodrugs, similarly as B13, affected also the cellular neutral and alkaline ceramidases, but with a low efficiency. Moreover, LCL521 acted as inhibitor of the lysosomal ACDase and ASMase whereas LCL522 and LCL596 may be specific to the lysosomal ACDase._x000D_ _x000D_ Reference: Bioorg Med Chem. 2014 Dec 15;22(24):6933-44. https://pubmed.ncbi.nlm.nih.gov/25456083/

The therapeutic benefit with adjuvant LCL521 was also achieved with SCCVII tumors treated with standard PDT when using immunocompetent mice but not with immunodeficient hosts. The interaction of LCL521 with PDT-based antitumor mechanisms is dominated by immune system contribution that includes overriding the effects of immunoregulatory cells, but could also include a tacit contribution from boosting direct tumor cell kill._x000D_ _x000D_ Reference: Int J Cancer. 2016 Sep 15;139(6):1372-8. https://pubmed.ncbi.nlm.nih.gov/27136745/

LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor.

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[1] Bai A, et al. Targeting (cellular) lysosomal acid ceramidase by B13: design, synthesis and evaluation of novel DMG-B13 ester prodrugs. Bioorg Med Chem. 2014 Dec 15;22(24):6933-44. DOI:10.1016/j.bmc.2014.10.025