GSK-LSD1 (hydrochloride) |
Catalog No.GC18012 |
LSD1 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2102933-95-7
Sample solution is provided at 25 µL, 10mM.
GSK-LSD1 (hydrochloride) is a potent, irreversible and mechanism-based inhibitor of LSD1 [1].
Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase existed in many transcriptional co-repressor complexes. LSD1 mediates H3K4 demethylation, causes a repressive chromatin environment which results in gene expression silence and has been shown to play a role in hematopoietic differentiation. It has been demonstrated that LSD1 is overexpressed in multiple tumor types [2].
In vitro: GSK-LSD1 inhibited the activity of LSD1 with an IC50 of 16 nM that is >1,000-fold selective over the closely related FAD-utilizing enzymes, such as LSD2, MAO-A, and MAO-B. GSK-LSD1 inhibited cell proliferation by inducing gene expression changes in various cancer cell lines, the EC50s were < 5 nM [1].
In vivo: In mice bearing LX44 or LX48, daily treatment with 1.5 mg/kg GSK-LSD1 showed 69% and 74% TGI, respectively [3].
References:
[1] Epigenetics probes collection. (2014).
[2] Smitheman K, Cusan M, Liu Y, et al. Inhibition of LSD1 for the treatment of cancer[J]. 2015.
[3] Mohammad H P, Smitheman K N, Kamat C D, et al. A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC[J]. Cancer Cell, 2015, 28(1): 57-69.
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