HDAC-IN-57

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC₅₀s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC₅₀ of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity^[1]. IC50 & Target:lysine-specific demethylase 1 (LSD1)^[1] IC50：1.34 μΜ(lysine-specific demethylase 1, LSD1) ^[1] In Vitro:HDAC-IN-57 (Compound 5e) (1.0 μM, 2.5 μM, 5.0 μΜ；48 hour) inhibits migration and invasion activity of MGC-803 and HCT-116 cells^[1].
HDAC-IN-57 (1.0 μM, 2.5 μM, 5.0 μΜ；48 hour) significantly inhibits the growth of solid tumor cell lines MGC-803, A549, and HCT-116, with IC₅₀s of 0.45 μM. 1.48 μM and 0.57 μM, respectively^[1].
HDAC-IN-57 (1.0 μM. 2.5 μM, 5.0 μΜ; 48 hours) triggers apoptosis of MGC-803 and HCT -116 cells in a dose-dependent manner^[1].
HDAC-IN-57 (1.0 μM. 2.5 μM, 5.0 μΜ; 48 hours) inhibits LSD1 and HDACs of MGC-803 and HCT -116 cells^[1].
HDAC-IN-57 (1.0 μM. 2.5 μM, 5.0 μΜ; 48 hours) induces G2/M cycle arrest in MGC-803 and HCT-116 cells^[1].
HDAC-IN-57 (Compound 5e) showes excellent metabolic stability in human liver (HLM) and rat liver microsomes (RLM), maintaining 86.1% and 87.4%, respectively, of the parent compound after incubation for 1 h, with T_1/2 values over 120 min^[1].
In Vivo:HDAC-IN-57 (Compound 5e) (1 mg.kg for i.v., 10 mg/kg for p.o.) shows a T_1/2 of 0.37 h (i.v.) and 2.75 h (p.o.), and oral bioavailability (F%) of 10.6%^[1].
HDAC-IN-57 (25 or 50 mg/kg, oral gavage once daily for 21 consecutive days) achieves a dose-dependent inhibition for tumor growth in an MGC-803 xenograft model with NOD-SCID mice^[1].
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