SR 11302

SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).

Product information

CAS Number: 160162-42-5

Molecular Weight: 376.53

Formula: C26H32O2

Chemical Name: (2E,4E,6Z,8E)-3-methyl-7-(4-methylphenyl)-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraenoic acid

Smiles: CC1CCCC(C)(C)C=1/C=C/C(=C/C=C/C(/C)=C/C(O)=O)/C1C=CC(C)=CC=1

InChiKey: RQANARBNMTXCDM-DKOHIBGUSA-N

InChi: InChI=1S/C26H32O2/c1-19-11-13-23(14-12-19)22(10-6-8-20(2)18-25(27)28)15-16-24-21(3)9-7-17-26(24,4)5/h6,8,10-16,18H,7,9,17H2,1-5H3,(H,27,28)/b8-6+,16-15+,20-18+,22-10-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (265.58 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SR 11302 (SR11302) show strong anti-AP-1 activity with selective binding with RARα and RARγ, but not with RARβ and RXRα. SR 11302 (SR-11302; 1 μM) inhibits AP-1 transcription factor activity and decreases aldosterone levels by 61.9% in hypoxia-treated cells. SR 11302 (SR-11302; 2 µM; 48 hours) inhibits Helicobacter pylori (H. pylori)-induced cell proliferation in adenocarcinoma gastric (AGS) cells. SR 11302 (2 µM; 24 hours) inhibits H. pylori-induced expression of β-catenin and c-myc in AGS cells.

In Vivo:

SR 11302 (SR11302; low dose 0.5 mg/kg and high dose 1 mg/kg body weight; orally gavaged daily) treatment reduces the total vascular lesion number and lesion size in Vldlr-/- mice in a dose-dependent manner.

References:

1. C Huang, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A. 1997 May 27;94(11):5826-30.
2. Bradley A Maron, et al. Upregulation of steroidogenic acute regulatory protein by hypoxia stimulates aldosterone synthesis in pulmonary artery endothelial cells to promote pulmonary vascular fibrosis. Circulation. 2014 Jul 8;130(2):168-79.
3. Eunyoung Byun, et al. Activation of NF-κB and AP-1 Mediates Hyperproliferation by Inducing β-Catenin and c-Myc in Helicobacter pylori-Infected Gastric Epithelial Cells. Yonsei Med J. 2016 May;57(3):647-51.

Products are for research use only. Not for human use.