Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
产品描述 | 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. |
体外活性 | S2116 is particularly effective for T-ALL cell lines with the IC 50 values between 1.1 μM for human T-ALL cell lines CEM and 6.8 μM for MOLT4[1]. S2116 (4-20 μM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes[1]. S2116 (4-8 μM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-ALL cells[1]. Cell Viability Assay[1]Cell Line: Normal T-lymphocytes Concentration: 4, 8, 12, 16, 20 μM Incubation Time: For 72 hours Result: Modestly inhibited mitogen-activated normal T-lymphocytes. Apoptosis Analysis[1]Cell Line: T-cell acute lymphoblastic leukemia (T-ALL) cells Concentration: 4, 6, 8 μM Incubation Time: For 24 hours Result: Induced apoptosis, as evidenced by increased annexin-V reactivity on flow cytometry in T-ALL cells in a dose- and time-dependent manner without affecting cell cycle distribution. Western Blot Analysis[1]Cell Line: T-ALL cells Concentration: 4, 6, 8 μM Incubation Time: For 24 hours Result: Down-regulated the expression of NOTCH3 and TAL1 proteins in T-ALL cells. |
体内活性 | S2116 (50 mg/kg; IP; 3 times a week; for 28 days) causes the size of subcutaneous tumors reduced to less than 20% of that in the untreated control[1]. S2116 (50 mg/kg; IP) has a T 1/2 of 3.76 hours, a C max of 12.7 μM and an AUC of 59.2 μM?h[1]. Animal Model: Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice with MOLT4 cells[1]Dosage: 50 mg/kg Administration: IP; 3 times a week; for 28 days Result: The size of subcutaneous tumors reduced to less than 20% of that in the untreated control. Animal Model: 8-week-old ICR mice[1]Dosage: 50 mg/kg (Pharmacokinetic Analysis) Administration: IP Result: Had a T 1/2 of 3.76 hours, a C max of 12.7 μM and an AUC of 59.2 μM?h. |
分子量 | 437.92 |
分子式 | C22H26ClF2N3O2 |
CAS No. | 2262489-89-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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