S2116

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

S2116 

S2116 是 N-烷基化的反式环丙胺 (TCP) 衍生物,是一种有效的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂。S2116 在超级增强子区域增加 H3K9 甲基化和相应的 H3K27 脱乙酰化。S2116 抑制 NOTCH3 和 TAL1 基因的转录,从而诱导 TCP 抵抗性急性淋巴细胞白血病 T-ALL 细胞凋亡 (apoptosis)。S2116 显着延迟异种移植小鼠中 T-ALL 细胞的生长。

S2116

S2116 Chemical Structure

CAS No. : 2262489-89-2

规格 价格 是否有货
5 mg ¥7500 询问价格 & 货期
10 mg ¥12000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice[1].

IC50 & Target

LSD1[1]

体外研究
(In Vitro)

S2116 is particularly effective for T-ALL cell lines with the IC50 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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 T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h.

分子量

437.91

Formula

C22H26ClF2N3O2

CAS 号

2262489-89-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Shiori Saito, et al. Eradication of Central Nervous System Leukemia of T-Cell Origin With a Brain-Permeable LSD1 Inhibitor. Clin Cancer Res. 2019 Mar 1;25(5):1601-1611.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务