HDACs/mTOR Inhibitor 1

HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC 50 s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1 , HDAC6 , mTOR , respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo . HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies In Vitro HDACs/mTOR Inhibitor 1 (Compound 12l) inhibits leukemia cells proliferation with IC 50 s of 4.05, 9.01, 9.98 μM for MV4-11, OCI-AML2, OCI-AML3 cells. HDACs/mTOR Inhibitor 1 (0-10 μM, 6 h or 24 h) downregulates p-ERK and increases Ac-H3 in MV4-11 cells. HDACs/mTOR Inhibitor 1 (10 to 1000 nM, 48 h) reduces S-phase cells and increases the percentage of cells in G0/G1 phase in MV4-11 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MV4-11 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 6 h or 24 h Result: Downregulated p-ERK (24 h) and increased of the Ac-H3 (6 h) in a dose-dependent manner. In Vivo HDACs/mTOR Inhibitor 1 (Compound 12l) (10 or 20 mg/kg, i.v.) inhibits tumor growth without significant toxicity in MV4-11 and MM1S xenograft NOD/SCID mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4-11 xenograft NOD/SCID mouse model Dosage: 10 mg/kg Administration: Intravenous injection (i.v.), every two days (Q2D)×6 Result: The TGI (tumor growth inhibitory rate) was 53.1%. IC50& Target:HDAC1 0.19 nM (IC 50 ) HDAC6 1.8 nM (IC 50 ) mTOR 1.2 nM (IC 50 )

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