WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406527
CAS#: 1172133-28-6
Description: HO-3867 is a selective and potent STAT3 inhibitor. HO-3867 selectively inhibited STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. HO-3867 exhibited minimal toxicity toward noncancerous cells and tissues but induced apoptosis in ovarian cancer cells. Pharmacologic analysis revealed greater bioabsorption and bioavailability of the active (cytotoxic) metabolites in cancer cells compared with normal cells. HO-3867 may be useful to treat ovarian cancer and other solid tumors where STAT3 is widely upregulated.
Hodoodo Cat#: H406527
Name: HO-3867
CAS#: 1172133-28-6
Chemical Formula: C28H30F2N2O2
Exact Mass: 464.23
Molecular Weight: 464.557
Elemental Analysis: C, 72.39; H, 6.51; F, 8.18; N, 6.03; O, 6.89
Synonym: HO3867; HO 3867; HO-3867.
IUPAC/Chemical Name: (3E,5E)-3,5-bis(4-fluorobenzylidene)-1-((1-hydroxy-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)methyl)piperidin-4-one
InChi Key: PWZQFTQMMAIRRM-JFMUQQRKSA-N
InChi Code: InChI=1S/C28H30F2N2O2/c1-27(2)15-23(28(3,4)32(27)34)18-31-16-21(13-19-5-9-24(29)10-6-19)26(33)22(17-31)14-20-7-11-25(30)12-8-20/h5-15,34H,16-18H2,1-4H3/b21-13+,22-14+
SMILES Code: O=C1/C(CN(CC2=CC(C)(C)N(O)C2(C)C)C/C1=C\C3=CC=C(F)C=C3)=C/C4=CC=C(F)C=C4
Appearance: white 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).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 464.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Rath KS, Naidu SK, Lata P, Bid HK, Rivera BK, McCann GA, Tierney BJ, Elnaggar AC, Bravo V, Leone G, Houghton P, Hideg K, Kuppusamy P, Cohn DE, Selvendiran K. HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27. doi: 10.1158/0008-5472.CAN-13-2433. Epub 2014 Mar 3. PubMed PMID: 24590057.
2: Ravi Y, Selvendiran K, Naidu SK, Meduru S, Citro LA, Bognár B, Khan M, Kálai T, Hideg K, Kuppusamy P, Sai-Sudhakar CB. Pulmonary hypertension secondary to left-heart failure involves peroxynitrite-induced downregulation of PTEN in the lung. Hypertension. 2013 Mar;61(3):593-601. doi: 10.1161/HYPERTENSIONAHA.111.00514. Epub 2013 Jan 21. PubMed PMID: 23339168; PubMed Central PMCID: PMC3747571.
3: Tierney BJ, McCann GA, Cohn DE, Eisenhauer E, Sudhakar M, Kuppusamy P, Hideg K, Selvendiran K. HO-3867, a STAT3 inhibitor induces apoptosis by inactivation of STAT3 activity in BRCA1-mutated ovarian cancer cells. Cancer Biol Ther. 2012 Jul;13(9):766-75. doi: 10.4161/cbt.20559. PubMed PMID: 22801507.
4: Selvendiran K, Ahmed S, Dayton A, Kuppusamy ML, Rivera BK, Kálai T, Hideg K, Kuppusamy P. HO-3867, a curcumin analog, sensitizes cisplatin-resistant ovarian carcinoma, leading to therapeutic synergy through STAT3 inhibition. Cancer Biol Ther. 2011 Nov 1;12(9):837-45. doi: 10.4161/cbt.12.9.17713. Epub 2011 Nov 1. PubMed PMID: 21885917.
5: Dayton A, Selvendiran K, Meduru S, Khan M, Kuppusamy ML, Naidu S, Kálai T, Hideg K, Kuppusamy P. Amelioration of doxorubicin-induced cardiotoxicity by an anticancer-antioxidant dual-function compound, HO-3867. J Pharmacol Exp Ther. 2011 Nov;339(2):350-7. doi: 10.1124/jpet.111.183681. Epub 2011 Jul 28. PubMed PMID: 21799049; PubMed Central PMCID: PMC3199994.
6: Dayton A, Selvendiran K, Kuppusamy ML, Rivera BK, Meduru S, Kálai T, Hideg K, Kuppusamy P. Cellular uptake, retention and bioabsorption of HO-3867, a fluorinated curcumin analog with potential antitumor properties. Cancer Biol Ther. 2010 Nov 15;10(10):1027-32. doi: 10.4161/cbt.10.10.13250. Epub 2010 Nov 15. PubMed PMID: 20798598; PubMed Central PMCID: PMC3047094.
7: Selvendiran K, Ahmed S, Dayton A, Ravi Y, Kuppusamy ML, Bratasz A, Rivera BK, Kálai T, Hideg K, Kuppusamy P. HO-3867, a synthetic compound, inhibits the migration and invasion of ovarian carcinoma cells through downregulation of fatty acid synthase and focal adhesion kinase. Mol Cancer Res. 2010 Sep;8(9):1188-97. doi: 10.1158/1541-7786.MCR-10-0201. Epub 2010 Aug 16. PubMed PMID: 20713491; PubMed Central PMCID: PMC2941821.
8: Selvendiran K, Tong L, Bratasz A, Kuppusamy ML, Ahmed S, Ravi Y, Trigg NJ, Rivera BK, Kálai T, Hideg K, Kuppusamy P. Anticancer efficacy of a difluorodiarylidenyl piperidone (HO-3867) in human ovarian cancer cells and tumor xenografts. Mol Cancer Ther. 2010 May;9(5):1169-79. doi: 10.1158/1535-7163.MCT-09-1207. Epub 2010 May 4. PubMed PMID: 20442315; PubMed Central PMCID: PMC2868073.
9: Selvendiran K, Ahmed S, Dayton A, Kuppusamy ML, Tazi M, Bratasz A, Tong L, Rivera BK, Kálai T, Hideg K, Kuppusamy P. Safe and targeted anticancer efficacy of a novel class of antioxidant-conjugated difluorodiarylidenyl piperidones: differential cytotoxicity in healthy and cancer cells. Free Radic Biol Med. 2010 May 1;48(9):1228-35. doi: 10.1016/j.freeradbiomed.2010.02.009. Epub 2010 Feb 12. PubMed PMID: 20156552; PubMed Central PMCID: PMC2847669.
10: Selvendiran K, Kuppusamy ML, Bratasz A, Tong L, Rivera BK, Rink C, Sen CK, Kálai T, Hideg K, Kuppusamy P. Inhibition of vascular smooth-muscle cell proliferation and arterial restenosis by HO-3867, a novel synthetic curcuminoid, through up-regulation of PTEN expression. J Pharmacol Exp Ther. 2009 Jun;329(3):959-66. doi: 10.1124/jpet.108.150367. Epub 2009 Mar 10. PubMed PMID: 19276401.
