HDAC-IN-53 

HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC₅₀ values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC₅₀>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer^[1].

HDAC-IN-53 (compound 19h) has good antiproliferative activity against a panel of cancer cell lines, for example MC38 (IC₅₀=0.66 μM), HCT116 cell (IC₅₀=0.56 μM) ^[1].
HDAC-IN-53 (0.1-1 μM; 24 h) causes G0/G1 cell cycle arrest in MC38 cells and induces G2/M cell cycle arrest in HCT116 cells^[1].
HDAC-IN-53 (0.1-1 μM; 24 h) upregulates the expressions of cleaved caspase-3 and cleaved PARP in a dose-dependent manner^[1].

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

HDAC-IN-53 (60 or 120 mg/kg; PO; daily for 15 days) exerts antitumor activities by both direct tumor growth inhibition and indirect immune cell-mediated antitumor effect^[1].
Pharmacokinetic Parameters of HDAC-IN-53 in Mice^[1].

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

461.90

C₂₃H₂₀ClN₇O₂

2921948-27-6

NC1=NN(C2=CC=CC=C2Cl)N=C1C(NCC3=CC=C(C=C3)C(NC4=CC=CC=C4N)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nan Sun, et al. Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response. J Med Chem. 2023 Apr 13;66(7):4802-4826.  [Content Brief]