LSD1-IN-24

Names

[ Name ]:
LSD1-IN-24

Biological Activity

[Description]:

LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Demethylase

Signaling Pathways >> Immunology/Inflammation >> PD-1/PD-L1

[In Vitro]

LSD1-IN-24 (compound 3S)(0-20 μM, 5 days) 可以以 LSD1 依赖性方式降低 PD-L1 水平并以剂量依赖性方式增强 BGC-823 细胞的 T 细胞杀伤反应，但不影响 BGC-823 和 MFC 细胞增殖。此外，它可以剂量依赖性地保护 H3K4me1/2 免于去甲基化，但不能保护 H3K4me3[1]。

[In Vivo]

LSD1-IN-24 (compound 3S) (0-50 mg/kg, oral gavage; daily for 2 weeks) 在含 MFC 细胞的皮下肿瘤模型中，以剂量依赖的方式抑制体内 MFC 细胞的生长，肿瘤的重量明显下降，肿瘤组织 Ki67 明显降低，并且对小鼠无明显毒性作用[1]。 Animal Model: Male 615 mice with MFC cell[1] Dosage: 0, 10, 25, and 50 mg/kg Administration: Oral gavage; daily for 2 weeks Result: Significantly decreased intratumoral PD-L1 expression, increased CD3+, CD4+, CD8+ cell numbers, interleukin-2 (IL2) and IFNγ mRNA and protein levels were also upregulated.

[References]

[1]. Xing-Jie Dai, et al. Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells. J Med Chem. 2023 Mar 23;66(6):3896-3916.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₂₀N₂OS

[ Molecular Weight ]:
312.43

Related Compounds

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