lysine specific demethylase-1 (lsd1)

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

Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth.

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.

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

(iso)-T 448 is a rotary isomer of T 448. T-448 is a potent lysine-specific demethylase 1 (LSD1) inhibitor that induces the methylation of H3K4 in rat neurons.

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

GSK 690 (Hydrochloride) is a reversible lysine-specific demethylase 1 (LSD1) inhibitor with a Kd of 9 nM and an IC50 of 37 nM.

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.

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.

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.

S 2101 is an inhibitor of lysine-specific demethylase 1 (LSD1)(IC50 of 0.99 μM, Ki of 0.61 μM and Kinact Ki of 4560 M s).

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

LSD1-IN-37 (Compound 5g) is an inhibitor of lysine-specific demethylase 1 (LSD1), developed through an efficient synthesis strategy incorporating a hexafluoroisopropyl group. This approach does not require metal catalysts and offers excellent reaction stability and adaptability. LSD1-IN-37 exhibits outstanding LSD1 inhibitory activity and has potential for further research.

LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 1.2 nM. It effectively inhibits the proliferation of cancer cells MV4-11, Kasumi-1, and NCI-H526 with IC50 values of 5, 4, and 11 nM, respectively. Furthermore, LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM and induces differentiation in MV4-11 cells. In mouse models, this compound demonstrates antitumor activity.

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

LSD1 HDAC6-IN-1 is an orally active dual inhibitor targeting lysine specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6), demonstrating promising anti-tumor activity, particularly valuable for multiple myeloma (MM) research [1].

Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.

Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also inhibits lysine-specific demethylase 1 (LSD1; IC50= 46.97 μM).3 1.Shidoji, Y., and Ogawa, H.Natural occurrence of cancer-preventive geranylgeranoic acid in medicinal herbsJ. Lipid Res.45(6)1092-1103(2004) 2.Shidoji, Y., Nakamura, N., Moriwaki, H., et al.Rapid loss in the mitochondrial membrane potential during geranylgeranoic acid-induced apoptosisBiochem. Biophys. Res. Commun.230(1)58-63(1997) 3.Sakane, C., Okitsu, T., Wada, A., et al.Inhibition of lysine-specific demethylase 1 by the acyclic diterpenoid geranylgeranoic acid and its derivativesBiochem. Biophys. Res. Commun.444(1)24-29(2014)

GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1) corepressor, with potential antineoplastic activity.

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.

S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted with T-ALL cells.

S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells when xenotransplanted into mice.

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.