lsd1/mao-b

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.

GSK-LSD1 dihydrochloride (GSK-LSD1 2HCl) is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD utilizing enzymes (i.e. MAO-A, LSD2, MAO-B).

OG-L002 hydrochloride is an effective and highly selective inhibitor of LSD1, with an IC50 of 0.02 µM. Additionally, it serves as an efficient monoamine oxidase (MAO) inhibitor, exhibiting IC50 values of 1.38 µM for MAO-A and 0.72 µM for MAO-B. This compound also effectively suppresses the expression of the HSV1E gene.

RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).

LSD1-IN-34 (Compound 7d) is an orally effective inhibitor of lysine-specific demethylase (LSD) and monoamine oxidase (MAO), exhibiting IC50 values of 4.51 nM for LSD1 and 18.46 nM for MAO A. This compound inhibits activation of neonatal rat cardiac fibroblasts (NRCF) induced by angiotensin II (Ang II) and shows no significant toxicity at 20 μM. LSD1-IN-34 also inhibits the TGFβ Smad signaling pathway, contributing to the improvement of heart failure in mice. Moreover, it demonstrates favorable pharmacokinetic properties in rats.

LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor that inhibits LSD1-CoREST, MAO-A, and MAO-B with IC50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 induces cell growth arrest in LNCaP cells of prostate cancer, with an IC50 value of 9.9 μM [1].

LSD1 HDAC6-IN-2 (JBI-802) is an orally effective inhibitor targeting LSD1, HDAC6, and MAO-A, demonstrating IC50 values of 5 nM, 11 nM, and 5 nM, respectively. This compound effectively suppresses the growth of multiple myeloma cells, including MM.1S, MM.1R, and RPMI-8226. Additionally, LSD1 HDAC6-IN-2 is utilized for researching acute myeloid leukemia and lymphoma.

LSD1-IN-17 (compound 5b) is a potent inhibitor of LSD1, effectively inhibiting LSD1-CoREST, MAO-A, and MAO-B with IC50 values of 0.005, 0.028, and 0.820 μM, respectively. It induces cell growth arrest in prostate cancer LNCaP cells with an IC50 value of 17.2 μM [1].

LSD1-IN-12 (compound 2) is an effective inhibitor of LSD1, with inhibitory Ki values of 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), and 3.5 μM (MAO-B) [1].

FY-56, a highly potent and selective inhibitor of LSD1 KDM1A with an IC50 value of 42 nM, demonstrates significant selectivity over MAO-A B. This compound effectively induces differentiation in MOLM-13 and MV4-11 cells, showing promise for acute myeloid leukemia (AML) research [1].

Vafidemstat (ORY-2001) is a selective, orally active lysyl-histone demethylase (LSD1) MAO-B inhibitor that crosses the blood-brain barrier for the study of neurological diseases.

OG-L002 is an effective and selective LSD1 inhibitor (IC50: 20 nM), showing 69- and 36-fold selectivity over MAO-A and MAO-B, respectively.

LSD1-IN-16 (compound 4b) is a potent inhibitor of LSD1 that inhibits LSD1-CoREST, MAO-A, and MAO-B with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 also induces cell growth arrest in prostate cancer LNCaP cells with an IC50 value of 15.2 μM [1].

LSD1-IN-26 (compound 12u), a potent LSD1 inhibitor, exhibits an IC50 of 25.3 nM. It also demonstrates inhibition of MAO-A (IC50 = 1234.57 nM) and MAO-B (IC50 = 3819.27 nM), significantly inducing apoptosis in MGC-803 cells. This compound is applicable in gastric cancer research [1].

Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.