product name GSK-LSD1 HCl
Description: GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, it is > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns. GSK-LSD1 induces gene expression changes in cancer cell lines (average EC50 < 5 nM) and inhibits cancer cell line growth (average EC50 < 5 nM).
References: http://www. thesgc.org/chemical-probes/LSD1.
289.24
Formula
C14H22Cl2N2
CAS No.
1431368-48-7(free base)
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: Soluble in DMSO
Water:
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: GSK-LSD1 induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM. Kinase Assay: Cell Assay: GSK-LSD1 2HCl irreversibly inhibited LSD1 with IC50 value of 16 nM and is > 1000 fold selective over LSD2, MAO-A and MAO-B, which were related to FAD utilizing enzymes. In cancer cell lines, GSK-LSD1 2HCl changed gene expression with average EC50 value < 5 nM and inhibited cells growth with average EC50 value < 5 nM. GSK-LSD1 2HCl (10 ?M) inhibited human recombinant dopamine transporter, 5-HT1A and 5-HT transporter by 39%, 49% and 74%, respectively. And no activity against other 55 recombinant receptors (GPCR, transporters, ion channels). GSK-LSD1 2HCl can be used as a chemical probe and a part of the SGC epigenetics. |
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| References |
