化合物 LSD1-IN-14 T61405

Product Introduction
Bioactivity


英文名: LSD1-IN-14

描述: LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].

体外活性: 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 IC 50 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 T 1/2 of 103.3 min and Cl int(mic) of 13.4 μL/min/mg [1]. 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.

体内活性: 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) C 0 (ng/mL) 575 C max (ng/mL) 41.1 T 1/2 (h) 1.0 T 1/2 (h) 2.8 Vd ss (L/kg) 6.6 T max (h) 0.8 Cl (mL/min/kg) 156 AUC 0-t (ng.h/mL) 126 AUC 0-t (ng.h/mL) 211 AUC 0-∞ (ng.h/mL) 152 AUC 0-∞ (ng.h/mL) 214 Bioacailability (%) 11.9 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

化合物 LSD1-IN-14 T61405信息由TargetMol中国为您提供，如您想了解更多关于化合物 LSD1-IN-14 T61405报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途