HDAC/Top-IN-1 

HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC₅₀s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy^[1].

HDAC/Top-IN-1 (compound 16j) (0-2 μM; 48 hours) exhibits remarkable inhibitory activities against the tested cell lines^[1].
HDAC/Top-IN-1 (20 and 100 nM; 24 hours) dramatically increases acetyl-H3 and acetyl-H4 levels in HEL cells^[1].
HDAC/Top-IN-1 (0.1 and 0.5 μM; 48 hours) effectively induces HEL cell apoptosis in a dose-dependent manner^[1].
HDAC/Top-IN-1 (0.02-0.5 μM; 48 hours) arrests HEL cells at the S phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC/Top-IN-1 exhibits good metabolic properties with a half-life (T_1/2) of 31.49 min, and the clearance is 173.32 mL/min/mg^[1].
HDAC/Top-IN-1 (5 and 10 mg/kg; PO; daily, for 14 days) exhibits potent oral antitumor activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

512.53

C₂₉H₂₅FN₄O₄

2411379-14-9

O=C1C2=C(N(C3N1CCC4=C3NC5=CC=C(OCC6=CC=C(C=C6)/C=C/C(NO)=O)C=C45)C)C=CC(F)=C2

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• [1]. Wu S, Huang Y, Wang T, et al. Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. J Med Chem. 2022;65(6):4818-4831.  [Content Brief]