LSD1-IN-14

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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。

LSD1-IN-14 

LSD1-IN-14 是一种有效且具有选择性的 LSD1 抑制剂 (IC50=0.89 μM)。LSD1-IN-14 能显著抑制 A549 和 THP-1 细胞的增殖，能诱导肿瘤细胞的凋亡。

LSD1-IN-14

LSD1-IN-14 Chemical Structure

CAS No. : 2698340-11-1

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生物活性

LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells[1].

IC50 & Target

IC50: 0.89 μM (LSD1)[1]
体外研究
(In Vitro)

LSD1-IN-14 (compound x43) (0-20 μM; 72 hours) has a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively[1].
LSD1-IN-14 (0-3 μM ;72 hours) significantly upregulates the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner[1].
LSD1-IN-14 (0-3 μM;72 hours) induces the apoptosis of 53.6% of A549 cells in a dose-dependent manner[1].
LSD1-IN-14 (1 mM; 60 minutes) has excellent stability in human liver microsomes and weak CYP inhibition, with T1/2 of 103.3 min and Clint(mic) of 13.4 μL/min/mg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549 and THP-1[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, respectively.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Significantly upregulated the expression of substrate H3K4me2 and H3K9me2 in a dose-dependent manner.

Apoptosis Analysis

Cell Line: A549 cells[1]
Concentration: 0, 0.3, 1 and 3 μM
Incubation Time: 72 hours
Result: Induced the apoptosis of 53.6% of cells in a dose-dependent manner.

体内研究
(In Vivo)

LSD1-IN-14 (2 mg/kg for i.v., 10 mg/kg for i.g, single) has an acceptable half-life and oral bioavailability[1].
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].

IV (2 mg/kg) IG (10 mg/kg)
C0 (ng/mL) 575 Cmax (ng/mL) 41.1
T1/2 (h) 1.0 T1/2 (h) 2.8
Vdss (L/kg) 6.6 Tmax (h) 0.8
Cl (mL/min/kg) 156 AUC0-t (ng.h/mL) 126
AUC0-t (ng.h/mL) 211 AUC0-∞ (ng.h/mL) 152
AUC0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 2 mg/kg for i.v., 10 mg/kg for i.g.
Administration: i.v. and i.g, single
Result: Showed an acceptable half-life and oral bioavailability.

分子量

365.45

Formula

C21H24FN5
CAS 号

2698340-11-1
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]. Wang X, et al. Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors. Bioorg Chem. 2022;121:105699.

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