A retinoid and an active metabolite of the retinoid etretinate that has antiproliferative activities; binds to CRABP-1 and CRABP-II (Kds = 3 and 15 nM

Acitretin – 10 mg

Brand:
Cayman
CAS:
55079-83-9
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Acitretin is a retinoid and an active metabolite of the retinoid etretinate (Item No. 19878) that has antiproliferative activities.{46411,46412} It binds to cellular retinoic acid binding protein I (CRABP-I) and CRABP-II (Kds = 3 and 15 nM, respectively, for the mouse recombinant proteins) but has low affinity for human recombinant retinoic acid receptor-retinoid X receptor (RAR-RXR) heterocomplexes.{46413,46414} Acitretin inhibits proliferation (IC50 = 6.6 µM) and suppresses TNF-α- and IFN-γ-induced protein levels of STAT1, NF-ĸB, and RANTES in HaCaT keratinocytes when used at concentrations up to 50 µM.{46415} It inhibits proliferation of HL-60, SCC4, SCC15, and A431, but not MCF-7, cancer cells, when used at a concentration of 30 µM.{46412} Acitretin (20 µg per mouse) decreases the severity of psoriatic-like skin lesions in K14-VEGF transgenic mice.{46411} Formulations containing acitretin have been used in the treatment of psoriasis.  

 

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Description

A retinoid and an active metabolite of the retinoid etretinate that has antiproliferative activities; binds to CRABP-1 and CRABP-II (Kds = 3 and 15 nM, respectively, for the mouse recombinant proteins) but has low affinity for human recombinant retinoic acid receptor-retinoid X receptor (RAR-RXR) heterocomplexes; inhibits proliferation (IC50 = 6.6 µM) and suppresses TNF-α- and IFN-γ-induced protein levels of STAT1, NF-ĸB, and RANTES in HaCaT keratinocytes when used at 50 µM; inhibits proliferation of HL-60, SCC4, SCC15, and A431, but not MCF-7, cancer cells, at 30 µM; decreases the severity of psoriatic-like skin lesions in K14-VEGF transgenic mice (20 µg per mouse)

Formal name: (2E,4E,6E,8E)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoic acid

Synonyms:  all-trans Acitretin|Ro 10-1670|Ro 10-1670/000

Molecular weight: 326.4

CAS: 55079-83-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Prenol Lipids||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cancer|Transcription Factors|STATs||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Lipid Biochemistry|Prenol Lipids

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