LSD1-IN-14

Name: LSD1-IN-14
Brand: TargetMol
SKU: T61405
Price: 233 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T61405Cas号 2698340-11-1

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].

LSD1-IN-14

还可以

产品编号 T61405Cas号 2698340-11-1

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].

规格	价格	库存
25 mg	¥ 10,600	6-8周
50 mg	¥ 13,800	6-8周
100 mg	¥ 17,500	6-8周

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产品介绍

生物活性

产品描述	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.