S2157 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。S2157 在超级增强子区域增加 H3K9 甲基化和相应的 H3K27 脱乙酰化。S2157 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)。S2157 有效地透过血脑屏障，几乎可以完全根除 T-ALL 细胞移植小鼠的中枢神经系统白血病。

S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.

Solid

LSD1

S2157 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.
S2157 (4-20 μM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes.
S2157 (4-8 μM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

S2157 (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.
S2157 (50 mg/kg; IP) has a T 1/2 of 0.88 hours, a C max of 4.33 μM and an AUC of 5.75 μM?h.
S2157 (30 mg/kg or 50 mg/kg; twice a week for 3 weeks) almost completely suppressed the growth of MOLT4 cells in most but not all NOD/SCID mice with MOLT4 cells. S2157 eradicates CNS leukemia in murine xenotransplanted models.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.