HDAC-IN-73 

HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC₅₀s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC₅₀=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer ^[1].

HDAC-IN-73 (compound P-503) (0-10 µM; 48 h) can inhibit proliferation of HCT116 cells with IC₅₀ value of 0.24 µM while PsA’s IC₅₀ value is 3.05 µM^[1].
HDAC-IN-73 (0.25-2 µM; 24 h) can increase the acetylation levels of histone H3 or α-tubulin in HCT116 cells comparing with PsA^[1].
HDAC-IN-73 (0.1-0.2 µM; 24 h) can induce apoptosis of HCT116 cells and has a superior proapoptotic effect to PsA^[1].
HDAC-IN-73(0.2-0.4 µM; 48 h) can induce HCT116 cell cycle arrest at G2 / M phase while PsA increases proportion of G1 phase^[1].

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

HDAC-IN-73 (compound P-503)(5 mg/kg; i.p.; every 2 days for 26 days) demonstrates a notable antitumor activity but also exists higher toxicity in HCT116 xenograft model in a 5 mg/kg dosage. The safety and toxic doses of HDAC-IN-73 needs further investigation^[1].

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

758.18

C₂₂H₂₄Br₂N₄O₆Se₂

2323571-16-8

OC1=CC=C(C/C(C(NCC[Se][Se]CCNC(/C(CC2=CC=C(O)C(Br)=C2)=N/O)=O)=O)=N\O)C=C1Br

Room temperature in continental US; may vary elsewhere.

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

• [1]. Jiang Y, et al. Psammaplin A analogues with modified disulfide bond targeting histone deacetylases: Synthesis and biological evaluation. Eur J Med Chem. 2024 May 31;275:116541.  [Content Brief]