lysine specific demethylase-1 (lsd1)

Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) 是一种有效的口服活性赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂，IC50为 0.25 nM，具有抗癌活性。它诱导急性髓细胞性白血病和小细胞肺癌细胞分化，对 LSD2、MOA-A 和 MAO-B 的酶抑制作用较小。

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

T-448 是一种可口服且具有高效性的赖氨酸特异性去甲基化酶1 抑制剂（IC50：22 nM），可改善小鼠的学习功能。T-448 可用于研究记忆缺陷。

Pulrodemstat (CC-90011) 是一种具有口服活性、选择性和高效性的赖氨酸特异性脱甲基酶-1 (LSD1) 抑制剂，具有抗癌抗肿瘤活性，抑制 HNSCC 细胞增殖和迁移，通过触发细胞凋亡来抑制头颈部鳞状细胞癌的生长。

Bomedemstat ditosylate (IMG-7289 ditosylate) 是一种具有口服活性的 lysine-specific demethylase 1 (LSD1) 抑制剂，具有抗肿瘤活性，增强 SCLC 同基因模型中对 PD-1 抑制的反应，抑制癌细胞增殖，诱导细胞凋亡。Bomedemstat ditosylate 可用于研究骨髓增生性肿瘤和骨髓纤维化。

Tranylcypromine hemisulfate (Tranylcypromine Sulfate) 是单胺氧化酶(MAO) 和赖氨酸特异性去甲基化酶 1 (LSD1) 的抑制剂，可用于研究抑郁症和子宫内膜异位症。

(iso)-T 448 是一种 T 448 的旋光异构体。T-448 是高效的赖氨酸特异性去甲基化酶1 (LSD1) 抑制剂，可诱导大鼠神经元中H3K4的甲基化。

GSK2879552 2HCl (1401966-69-5(free base)) 是一种口服的、不可逆的赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂，具有潜在的抗肿瘤活性。

GSK 690 (Hydrochloride) 是一种可逆的赖氨酸特异性去甲基化酶1 (LSD1)抑制剂，Kd 值为 9 nM，IC50值为 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.

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

LSD1-IN-37 (Compound 5g) 是赖氨酸特异性去甲基化酶 1 (LSD1) 的一种抑制剂，通过高效合成策略构建而成，该策略包含六氟异丙基基团并无需金属催化剂。此方法展现出良好的反应稳定性和适应性。LSD1-IN-37 表现出杰出的LSD1抑制活性，具有进一步研究的潜力。

LSD1-IN-38 (Compound 23e) 是一种具有口服活性的可逆性赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂，IC50为 1.2 nM。该化合物能有效抑制癌细胞MV4-11、Kasumi-1和NCI-H526的增殖，其IC50分别为5 nM、4 nM和11 nM。LSD1-IN-38 还能够激活CD86的表达，EC50为0.034 μM，促进MV4-11细胞分化。在小鼠模型中，LSD1-IN-38 展示了明显的抗肿瘤活性。

RN-1 dihydrochloride 是血脑屏障通透性的、不可逆的赖氨酸特异性脱甲基酶 1 (LSD1) 选择性抑制剂，IC50为 70 nM，对 LSD1 的选择性高于 MAO-A 和 MAO-B，IC50分别为 0.51 μM 和 2.785 μM。

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].

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 是一种选择性的、可口服的、不可逆的、基于机制的赖氨酸特异性去甲基化酶 1 (LSD1) 辅阻遏物灭活剂，具有潜在的抗肿瘤活性。

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.