LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.

Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

GSK-LSD1, an LSD1 inhibitor, decreases food consumption and body weight while enhancing insulin sensitivity and glycemic regulation in murine obesity models. Additionally, it mitigates non-alcoholic fatty liver disease (NAFLD) and suppresses cytokine release induced by SARS-CoV-2 in COVID-19 peripheral blood mononuclear cells (PBMCs). Furthermore, GSK-LSD1 inhibits the proliferation and spread of cancer [1] [2] [3].

LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.

LSD1-IN-30 is a lysine-specific demethylase 1 (LSD1) inhibitor with anticancer activity for the study of small cell lung cancer and acute myeloid leukemia.

LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].

LSD1-IN-25 (Compound 9j) is a potent, selective, and orally active inhibitor of LSD1, exhibiting an IC50 of 46 nM (Ki = 30.3 nM) and capable of inducing apoptosis in cancer cells [1].

LSD1-IN-13 hydrochloride (compound 7e) is an orally active inhibitor of LSD1 (IC50: 24.43 nM). hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines.

LSD1-IN-18 is a potent, non-covalent, selective inhibitor of LSD1 (Ki:0.156 μM; KD: 0.075 μM).LSD1-IN-18 exhibited anti-proliferative effects in THP-1 leukemia cells and MDA-MB-231 breast cancer cells with IC50 (72 h) of 0.16 and 0.21 μM, respectively.

LSD1-UM-109 is a highly potent and reversible inhibitor of LSD1, demonstrating an IC50 of 3.1 nM. This compound exhibits strong antiproliferative activity, inhibiting cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line [1].

LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor that inhibit LSD1-CoREST, MAO-A and MAO-B with IC 50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 shows cell growth arrest in LNCaP cells of prostate cancer. The IC50 value is 9.9 μM [1].

LSD1/ER-IN-1 (compound 11g) is a potent inhibitor of ER and LSD1 that acts on LSD1 (IC50: 1.55 μM). LSD1/ER-IN-1 showed good anti-proliferative effect on MCF-7 breast cancer cells (IC50: 8.79 μM).

LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 ( LSD1 ) with a Ki value of 11 nM rather than 7 μM for LSD2. There is aberrant expression of LSD1 in tumor stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation [1].

LSD1-IN-17 (compound 5b) is a potent inhibitor of LSD1 that inhibits LSD1-CoREST, MAO-A and MAO-B, with IC 50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 exhibits cell growth arrest in prostate cancer LNCaP cells with an IC50 value of 17.2 μM [1].

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).

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 exhibits 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].

LSD1-IN-19 (compound 29) is a selective, potent, non-covalent inhibitor of LSD1 (Ki: 0.108 μM, KD: 0.068 μM). The 72h IC50 values were 0.17 and 0.40 μM, respectively.

LSD1/2-IN-4, a derivative of PCPA, functions as an inhibitor for both lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2), demonstrating K i values of 0.11 μM and 130 μM against LSD1 and LSD2, respectively. This compound is utilized in researching various cancers, notably T-cell acute lymphoblastic leukemia (TALL) [1].

LSD1-IN-22 is a potent inhibitor of Lysine-specific demethylase 1 ( LSD1 ) with a K i value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells [1].

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

LSD1/HDAC6-IN-1 is an orally active compound that functions as a dual inhibitor, targeting lysine specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6). This compound demonstrates promising anti-tumor activity and is particularly valuable for research focused on multiple myeloma (MM) [1].

LSD1-IN-13 (compound 7e) is an orally active LSD1 inhibitor (IC50: 24.43 nM) that also activates CD86 expression (EC50: 470 nM).LSD1-IN-13 induces differentiation of AML (acute myeloid leukaemia) cell lines.

LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-6 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM.

LSD1-IN-21 is a potent, blood-brain barrier permeable LSD1 (lysine specific demethylase-1) inhibitor (IC50: 0.956 μM).LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α and exhibits good anti-cancer and anti-inflammatory effects.

LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-5 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM.

Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.

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

LSD1-IN-7 Methylbenzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.

Corin is an irreversible inhibitor of HDAC1(IC50 = 147 nM) and LSD1(Ki = 110 nM).

DDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor (IC50: 84 nM).

Bomedemstat ditosylate (IMG-7289 ditosylate) is an orally active lysine-specific demethylase 1 (LSD1) inhibitor with antitumor activity that potentiates the response to PD-1 inhibition in a homozygous model of SCLC, inhibits cancer cell proliferation, and induces apoptosis. Bomedemstat ditosylate can be used to study myeloproliferative neoplasms and myelofibrosis.

TPC-144 is a potent and selective LSD1 inhibitor with a reversible inhibition mechanism. TPC-144 has antitumor activity in several human AML and SCLC cell lines and xenograft models.

T-448 is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).

TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.

ORY1001 (ORY 1001) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor, with high selectivity against related FAD dependent aminoxidases with IC50 of <20 nM.

T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).

INCB059872 is a highly potent, orally active, selective, and irreversible inhibitor of Lysine-Specific Demethylase 1 (LSD1). Its chemical properties make it suitable for use in researching myeloid leukemia.

MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and suppressing cell migration, thus showing potential for use in gastric cancer research [1].

CBB1007 Hcl is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

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

Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.

Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.

NCD38 TFA serves as a selective inhibitor of LSD1 [1] [2].

cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells [1].

Namoline is a γ-pyrone compound that functions as a selective and reversible inhibitor of Lysine-specific demethylase 1 (LSD1) with an IC50 of 51 μM in an HRP-coupled enzymatic assay. By impairing LSD1 demethylase activity, Namoline effectively inhibits cell proliferation. Due to its characteristics, Namoline holds promise for research pertaining to androgen-dependent prostate cancer.

Domatinostat tosylate (4SC-202) is a selective inhibitor of class I HDAC for HDAC1/2/3 (IC50: 1.20/1.12/0.57 μM). It also displays inhibitory activity against Lysine-specific demethylase 1 (LSD1).