LSD1-IN-13

Names

[ CAS No. ]:
2170212-33-4

[ Name ]:
LSD1-IN-13

Biological Activity

[Description]:

LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Demethylase

[Target]

IC50: 24.43 ± 1.08 nM (LSD1), 5.00 ± 0.28 μM (LSD2), >100 μM (MAO-A), >100 μM (MAO-B)[1]


[In Vitro]

LSD1-IN-13 (compound 7e) shows good selectivity over LSD2 (205-fold) and MAOs (>4000-fold)[1]. LSD1-IN-13 shows potent and selective antiproliferative activity in MV-4-11, with an IC50 of 1.36 μM[1].

[In Vivo]

LSD1-IN-13 (compound 7e) (MV-4-11 xenograft mice, 0-20 mg/kg, Orally, daily for 15 days) suppresses tumor growth significantly in a dose-dependent manner[1].

[References]

[1]. Li C, et al. Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors. J Med Chem. 2022 Mar 10;65(5):4335-4349.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H29N3O2S

[ Molecular Weight ]:
411.56

Related Compounds