| 产品描述: | 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. |
| 体外研究: |
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]. |
| 体内研究: |
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. S2116 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes. S2116 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-ALL cells. |
| 保存条件: |
2-8°C, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.284 ml |
11.418 ml |
22.835 ml |
| 5 mM |
0.457 ml |
2.284 ml |
4.567 ml |
| 10 mM |
0.228 ml |
1.142 ml |
2.284 ml |
| 50 mM |
0.046 ml |
0.228 ml |
0.457 ml |
|
| 注意: |
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