10058-F4
10058-F4 is a potent and selective c-Myc inhibitor, which markedly increases valproic acid-induced cell death in Jurkat and CCRF-CEM T-lymphoblastic leukemia cells. 10058-F4 inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells. 10058-F4 induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia.
1: Zhang M, Fan HY, Li SC. Inhibition of c-Myc by 10058-F4 induces growth arrest and chemosensitivity in pancreatic ductal adenocarcinoma. Biomed Pharmacother. 2015 Jul;73:123-8. doi: 10.1016/j.biopha.2015.05.019. Epub 2015 Jun 1. PubMed PMID: 26211592.
2: Mu Q, Ma Q, Lu S, Zhang T, Yu M, Huang X, Chen J, Jin J. 10058-F4, a c-Myc inhibitor, markedly increases valproic acid-induced cell death in Jurkat and CCRF-CEM T-lymphoblastic leukemia cells. Oncol Lett. 2014 Sep;8(3):1355-1359. Epub 2014 Jun 24. PubMed PMID: 25120723; PubMed Central PMCID: PMC4114592.
3: Guo J, Parise RA, Joseph E, Egorin MJ, Lazo JS, Prochownik EV, Eiseman JL. Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice. Cancer Chemother Pharmacol. 2009 Mar;63(4):615-25. doi: 10.1007/s00280-008-0774-y. Epub 2008 May 29. PubMed PMID: 18509642; PubMed Central PMCID: PMC2752825.
4: Lin CP, Liu JD, Chow JM, Liu CR, Liu HE. Small-molecule c-Myc inhibitor, 10058-F4, inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells. Anticancer Drugs. 2007 Feb;18(2):161-70. PubMed PMID: 17159602.
5: Huang MJ, Cheng YC, Liu CR, Lin S, Liu HE. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia. Exp Hematol. 2006 Nov;34(11):1480-9. PubMed PMID: 17046567.
| Chemical | |
|---|---|
| CAS Num | 403811-55-2 |
| Chemical Formula | C12H11NOS2 |
| Molecular Weight | 249.346 |
| IUPAC Chemical Name | 5-[(4-ethylphenyl)methylene]-2-thioxo-4-thiazolidinone |
| Exact Mass | 249.0282 |
| Elemental Analysis | C, 57.80; H, 4.45; N, 5.62; O, 6.42; S, 25.72 |
| Synonym | 10058-F4; 10058F4; 10058 F4. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C1NC(S/C1=C/C2=CC=C(CC)C=C2)=S |
| Biological | |
| Targets and Effects | c-Myc inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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