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| | SR 11302 Basic information |
| Product Name: | SR 11302 | | Synonyms: | SR 11302;(E,E,Z,E)-3-Methyl-7-(4-methylphenyl)-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenoicacid;RQANARBNMTXCDM-DKOHIBGUSA-N;2,4,6,8-Nonatetraenoic acid, 3-methyl-7-(4-methylphenyl)-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-, (2E,4E,6Z,8E)-;(2E,4E,6Z,8E)-3-Methyl-7-(p-tolyl)-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraenoic acid;acid,SR11302,retinoid,SR-11302,Lung,RARE,Cancer,response,Inhibitor,protein-1,SR 11302,inhibit,AP-1,retinoic,element,activator;SR 11302, 10 mM in DMSO;(E,E,Z,E)-3-Methyl-7-(4-methylphenyl)-9-(2,6,6-trimethylcyclohex-1-en-1-yl) nona-2,4,6,8-tetraenoic acid | | CAS: | 160162-42-5 | | MF: | C26H32O2 | | MW: | 376.53 | | EINECS: | | | Product Categories: | | | Mol File: | 160162-42-5.mol |  |
| | SR 11302 Chemical Properties |
| Boiling point | 541.6±30.0 °C(Predicted) | | density | 1.048±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | crystalline solid | | pka | 4.67±0.33(Predicted) | | color | Light yellow to yellow |
| | SR 11302 Usage And Synthesis |
| Description | The receptors for retinoids, RARs and RXRs, induce transcriptional activation by binding the specific retinoid response elements, RARE and RXRE. Alternatively, retinoid receptors interact with and modulate other transcription factors, including activator protein-1 (AP-1). SR 11302 is a synthetic retinoid that inhibits AP-1 activity without activating transcription through RARE. It significantly suppresses both AP-1 activation and phorbol ester-induced papilloma formation in mice when applied topically (0.1 μM). SR 11302 is used to elucidate the role of AP-1 in various signaling pathways. | | Uses | SR 11302 is an inhibitor of activator protein-1. | | Biological Activity | Inhibitor of activator protein-1 (AP-1) transcription factor activity that displays antitumor effects in vivo . Does not activate transcription from the retinoic acid response element (RARE) and displays no activity at retinoic acid receptors (EC 50 > 1 μ M for RAR α , RAR β , RAR γ and RXR α ). | | 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[4]. | Animal Model: | Vldlr-/- mice[4] | | Dosage: | Low dose 0.5 mg/kg and high dose 1 mg/kg body weight | | Administration: | Orally gavaged daily from P5 to P15 | | Result: | High-dose from P5 to P15 reduced the total vascular lesion number by 48% and decreased the lesion size by 40%, without detectable signs of toxicity in mice, including no change in body weight. |
| | storage | Store at -20°C | | References | [1] MD M D. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation[J]. Journal of the American Academy of Dermatology, 1995, 33 1: Page 109. DOI: 10.1016/0190-9622(95)90031-4
[2] C HUANG. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1997, 94 11: 5826-5830. DOI: 10.1073/pnas.94.11.5826
[3] M SHIOHARA. Effects of novel RAR- and RXR-selective retinoids on myeloid leukemic proliferation and differentiation in vitro.[J]. Blood, 1999, 93 6: 2057-2066.
[4] HANNU KANKAANRANTA. Tumour necrosis factor-α regulates human eosinophil apoptosis via ligation of TNF-receptor 1 and balance between NF-κB and AP-1.[J]. PLoS ONE, 2014: e90298. DOI: 10.1371/journal.pone.0090298 |
| | SR 11302 Preparation Products And Raw materials |
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