LSD1 Inhibitor II, S2101-Calbiochem

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一般描述

A cell-permeable, 2-PCPA derivative that elicits mechanism based inhibition of LSD1 (IC₅₀= 0.99 ?M, K_I= 0.61 ?M, and k_inact/K_I= 4560 (M^-1S^-1)), and displays much lower inhibition activity toward MAO-B (K_I= 17 ?M, k_inact/K_I= 18 (M^-1S^-1)) and MAO-A inhibition (K_I= 110 ?M, k_inact/K_I= 60 (M^-1S^-1)), with higher potency and selectivity compared with 2-PCPA, IC₅₀= 184 ?M, K_I= 100 ?M, k_inact/K_I= 58 (M^-1S^-1)) for LSD1, and K_I= 26 ?M, k_inact/K_I= 271 (M^-1S^-1)) for MAO-B, and K_I= 5 ?M, k_inact/K_I= 1050 (M^-1S^-1)) for MAO-A). The inhibition of LSD1 is further confirmed in a cell based assay, the treatment of HEK293T human cells with S2101 results in a dose-dependent increase in the level of H3K4me2, and about 50-fold stronger inhibition compared with that of 2-PCPA.
A cell-permeable, 2-PCPA derivative that elicits mechanism-based inhibition against LSD1 (IC₅₀= 0.99 ?M, K_I= 0.61 ?M, and k_inact/K_I= 4560 M^-1S^-1), and displays much lower inhibition activity toward MAO-B (K_I= 17 ?M, k_inact/K_I= 18 M^-1S^-1) and MAO-A (K_I= 110 ?M, k_inact/K_I= 60 M^-1S^-1), with higher potency and selectivity compared with those of 2-PCPA (Cat. No. 616431) (IC₅₀= 184 ?M, K_I= 100 ?M, k_inact/K_I= 58 M^-1S^-1for LSD1, and K_I= 26 ?M, k_inact/K_I= 271 M^-1S^-1for MAO-B, and K_I= 5 ?M,
k_inact/K_I= 1050 M^-1S^-1for MAO-A). The inhibition of LSD1 is further confirmed in a cell-based assay, the treatment of HEK293T human cells with S2101 results in a dose-dependent increase in the level of H3K4me2, and about 50-fold stronger inhibition compared with that of 2-PCPA.

包装

5 mg in Glass bottle

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Mimasu, S., et al. 2010.Biochemistry49,6494.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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