For research use only. Not for therapeutic Use.
DIM-C-pPhOH（Cat No.:I014337）, also known as C-DIM8 or CDIM8, is a potent antagonist of the nuclear receptor 4A1 (NR4A1), It exhibits inhibitory effects on tumor growth and mTOR signaling, while inducing apoptosis and cellular stress. DIM-C-pPhOH has demonstrated the ability to reduce cell proliferation, with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively. These properties highlight the potential of DIM-C-pPhOH as a therapeutic agent for targeting NR4A1 and inhibiting tumor growth.
| Catalog Number | I014337 |
| CAS Number | 151358-47-3 |
| Synonyms | DIM-C-pPhOH;1,1-Bis(3′-indolyl)-1-(p-hydroxyphenyl)methane |
| Molecular Formula | C23H18N2O |
| Purity | ≥95% |
| Target | Apoptosis |
| Solubility | Soluble in DMSO |
| Storage | Room Temperature |
| IUPAC Name | 4-[bis(1H-indol-3-yl)methyl]phenol |
| InChI | InChI=1S/C23H18N2O/c26-16-11-9-15(10-12-16)23(19-13-24-21-7-3-1-5-17(19)21)20-14-25-22-8-4-2-6-18(20)22/h1-14,23-26H |
| InChIKey | QCPDFNWJBQMXLI-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C(=C1)C(=CN2)C(C3=CC=C(C=C3)O)C4=CNC5=CC=CC=C54 |
| Reference | </br> 1: Hedrick E, Lee SO, Safe S. The nuclear orphan receptor NR4A1 regulates β1-integrin expression in pancreatic and colon cancer cells and can be targeted by NR4A1 antagonists. Mol Carcinog. 2017 Sep;56(9):2066-2075. doi: 10.1002/mc.22662. Epub 2017 May 9. PubMed PMID: 28418095; PubMed Central PMCID: PMC5546981.</br>2: Jiang Y, Zeng Y, Huang X, Qin Y, Luo W, Xiang S, Sooranna SR, Pinhu L. Nur77 attenuates endothelin-1 expression via downregulation of NF-κB and p38 MAPK in A549 cells and in an ARDS rat model. Am J Physiol Lung Cell Mol Physiol. 2016 Dec 1;311(6):L1023-L1035. doi: 10.1152/ajplung.00043.2016. Epub 2016 Oct 7. PubMed PMID: 27765761; PubMed Central PMCID: PMC5206403.</br>3: Lacey A, Hedrick E, Li X, Patel K, Doddapaneni R, Singh M, Safe S. Nuclear receptor 4A1 (NR4A1) as a drug target for treating rhabdomyosarcoma (RMS). Oncotarget. 2016 May 24;7(21):31257-69. doi: 10.18632/oncotarget.9112. PubMed PMID: 27144436; PubMed Central PMCID: PMC5058754.</br>4: Hedrick E, Lee SO, Doddapaneni R, Singh M, Safe S. NR4A1 Antagonists Inhibit β1-Integrin-Dependent Breast Cancer Cell Migration. Mol Cell Biol. 2016 Apr 15;36(9):1383-94. doi: 10.1128/MCB.00912-15. Print 2016 May. Erratum in: Mol Cell Biol. 2017 Aug 28;37(18):. PubMed PMID: 26929200; PubMed Central PMCID: PMC4836213.</br>5: Hedrick E, Lee SO, Doddapaneni R, Singh M, Safe S. Nuclear receptor 4A1 as a drug target for breast cancer chemotherapy. Endocr Relat Cancer. 2015 Oct;22(5):831-40. doi: 10.1530/ERC-15-0063. Epub 2015 Jul 30. PubMed PMID: 26229035.</br>6: Hedrick E, Lee SO, Kim G, Abdelrahim M, Jin UH, Safe S, Abudayyeh A. Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma. PLoS One. 2015 Jun 2;10(6):e0128308. doi: 10.1371/journal.pone.0128308. eCollection 2015. PubMed PMID: 26035713; PubMed Central PMCID: PMC4452731.</br>7: De Miranda BR, Popichak KA, Hammond SL, Miller JA, Safe S, Tjalkens RB. Novel para-phenyl substituted diindolylmethanes protect against MPTP neurotoxicity and suppress glial activation in a mouse model of Parkinson’s disease. Toxicol Sci. 2015 Feb;143(2):360-73. doi: 10.1093/toxsci/kfu236. Epub 2014 Nov 17. PubMed PMID: 25406165; PubMed Central PMCID: PMC4306720.</br>8: Lee SO, Li X, Hedrick E, Jin UH, Tjalkens RB, Backos DS, Li L, Zhang Y, Wu Q, Safe S. Diindolylmethane analogs bind NR4A1 and are NR4A1 antagonists in colon cancer cells. Mol Endocrinol. 2014 Oct;28(10):1729-39. doi: 10.1210/me.2014-1102. Epub 2014 Aug 6. PubMed PMID: 25099012; PubMed Central PMCID: PMC4179635.</br>9: Lee SO, Jin UH, Kang JH, Kim SB, Guthrie AS, Sreevalsan S, Lee JS, Safe S. The orphan nuclear receptor NR4A1 (Nur77) regulates oxidative and endoplasmic reticulum stress in pancreatic cancer cells. Mol Cancer Res. 2014 Apr;12(4):527-538. doi: 10.1158/1541-7786.MCR-13-0567. Epub 2014 Feb 10. PubMed PMID: 24515801; PubMed Central PMCID: PMC4407472.</br>10: Andey T, Patel A, Jackson T, Safe S, Singh M. 1,1-Bis (3′-indolyl)-1-(p-substitutedphenyl)methane compounds inhibit lung cancer cell and tumor growth in a metastasis model. Eur J Pharm Sci. 2013 Oct 9;50(2):227-41. doi: 10.1016/j.ejps.2013.07.007. Epub 2013 Jul 23. PubMed PMID: 23892137; PubMed Central PMCID: PMC3838903.</br>11: Lee SO, Andey T, Jin UH, Kim K, Singh M, Safe S. The nuclear receptor TR3 regulates mTORC1 signaling in lung cancer cells expressing wild-type p53. Oncogene. 2012 Jul 5;31(27):3265-76. doi: 10.1038/onc.2011.504. Epub 2011 Nov 14. Erratum in: Oncogene. 2012 Jul 5;31(27):3310. Sachdeva, M [corrected to Singh, M]. PubMed PMID: 22081070; PubMed Central PMCID: PMC3299891.</br>12: Lee SO, Li X, Khan S, Safe S. Targeting NR4A1 (TR3) in cancer cells and tumors. Expert Opin Ther Targets. 2011 Feb;15(2):195-206. doi: 10.1517/14728222.2011.547481. Epub 2011 Jan 5. Review. PubMed PMID: 21204731; PubMed Central PMCID: PMC4407471.</br>13: Lee SO, Abdelrahim M, Yoon K, Chintharlapalli S, Papineni S, Kim K, Wang H, Safe S. Inactivation of the orphan nuclear receptor TR3/Nur77 inhibits pancreatic cancer cell and tumor growth. Cancer Res. 2010 Sep 1;70(17):6824-36. doi: 10.1158/0008-5472.CAN-10-1992. Epub 2010 Jul 21. PubMed PMID: 20660371; PubMed Central PMCID: PMC2988472. </br> </br> |
