| Description |
LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells[1].
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| Related Catalog |
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| Target |
IC50: 0.89 μM (LSD1)[1]
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| In Vitro |
LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively[1]. LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner[1]. LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner[1]. LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg[1]. Cell Proliferation Assay Cell Line: A549 and THP-1[1] Concentration: 0-20 μM Incubation Time: 72 hours Result: Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively. Western Blot Analysis Cell Line: A549 cells[1] Concentration: 0, 0.3, 1 and 3 μM Incubation Time: 72 hours Result: Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner. Apoptosis Analysis Cell Line: A549 cells[1] Concentration: 0, 0.3, 1 and 3 μM Incubation Time: 72 hours Result: Induced the apoptosis of 53.6% of cells in a dose-dependent manner.
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| In Vivo |
LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability[1]. Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1]. IV (2 mg/kg) IG (10 mg/kg) C0 (ng/mL) 575 Cmax (ng/mL) 41.1 T1/2 (h) 1.0 T1/2 (h) 2.8 Vdss (L/kg) 6.6 Tmax (h) 0.8 Cl (mL/min/kg) 156 AUC0-t (ng.h/mL) 126 AUC0-t (ng.h/mL) 211 AUC0-∞ (ng.h/mL) 152 AUC0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9 Animal Model: Male Sprague-Dawley rats[1] Dosage: 2 mg/kg for i.v., 10 mg/kg for i.g. Administration: i.v. and i.g, single Result: Showed an acceptable half-life and oral bioavailability.
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| References |
[1]. Wang X, et al. Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors. Bioorg Chem. 2022;121:105699.
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