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编 号:F758392
分子式:C18H20N2OS
分子量:312.43
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体内研究:
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。Animal Model:Male 615 mice with MFC cell
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.

体外研究:
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。
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