Peretinoin  (Synonyms: NIK333)

Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1^[1]. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression^[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC₅₀ of 9 μM^[3].

Peretinoin (10-40 μM; 12-72 hours) exhibits suppressed SPHK1 expression after 24 h treatment, even at 10 μM and more prominent after 72 h peretinoin treatment ^[1].
Peretinoin (5 μM; 24 hours) up-regulates the expression of LC3B-II and increases autophagy flux in mouse primary hepatocytes^[2].

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

302.45

Solid

C₂₀H₃₀O₂

81485-25-8

C/C(C)=C/CC/C(C)=C/CC/C(C)=C/C=C/C(C)=C/C(O)=O

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Honda M, et al. Peretinoin, an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. BMC Cancer. 2013 Apr 15;13:191.  [Content Brief]

  [2]. Okada H, et al. Peretinoin, an acyclic retinoid, suppresses steatohepatitis and tumorigenesis by activating autophagy in mice fed an atherogenic high-fat diet. Oncotarget. 2017 Jun 20;8(25):39978-39993.  [Content Brief]

  [3]. Funaki M, et al. Peretinoin, an acyclic retinoid, inhibits hepatocarcinogenesis by suppressing sphingosine kinase 1 expression in vitro and in vivo. Sci Rep. 2017 Dec 5;7(1):16978.  [Content Brief]