Benzenepropanamide, N,N′-(diselenodi-2,1-ethanediyl)bis[3-bromo-4-hydroxy-α-(hydroxyimino)-, (αE,α′E)-

Product NameBenzenepropanamide, N,N′-(diselenodi-2,1-ethanediyl)bis[3-bromo-4-hydroxy-α-(hydroxyimino)-, (αE,α′E)-
CAS2323571-16-8
MFC22H24Br2N4O6Se2
MW758.18
EINECS
MOL File2323571-16-8.mol

Chemical Properties

pka	7.85±0.20(predicted)

Usage And Synthesis

Uses

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].

in vivo

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].

Animal Model:	6 weeks, Female nude mice (BALB/c-nu) (HCT116 xenograft model)^[1]
Dosage:	5 mg/kg
Administration:	I.p.; every 2 days for 26 days
Result:	Reduced the tumor volume (p < 0.0001) and the tumor weight (p < 0.01). Exhibited the significant loss of body weight which has the same trend with the group of negative control. Inhibited the tumor growth (TGI = 74.6 %) , while the TGI of SAHA (10 mg/kg, positive control) and PsA (10 mg/kg) were 13.1 % and 36.1 %, respectively. Existed high toxicity, 2 mice died during the medication. Western blot tests showed that the acetylation levels of histone H3 or α-tubulin in tumor tissues were up-regulated.

IC 50

HDAC1: 0.17 μM (IC₅₀); HDAC6: 0.49 μM (IC₅₀)

References

[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. DOI:10.1016/j.ejmech.2024.116541

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