HO-3867 | CAS#1172133-28-6 | STAT3 inhibitor

HO-3867
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406527

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.

Chemical Structure

HO-3867

CAS# 1172133-28-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406527
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

Price and Availability

Size	Price	Availability
5mg	USD 250	2 Weeks
10mg	USD 400	2 Weeks
25mg	USD 700	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

Product Data:

Product Data

Instruction:

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Biological target:	HO-3867 is a selective and potent STAT3 inhibitor.
In vitro activity:	After treatment with HO-3867 for 24 h, U2OS, HOS, and MG-63 cells’ viability in concentrations of 2, 4, 8, 16, and 32 μM of HO-3867 was significantly unlike that of controls (0 μM) and showed dose-dependently (U2OS: p < 0.001; HOS: p < 0.001; MG-63: p < 0.001). (Figure 1B) After 24 h of HO-3867 (4, 8, and 16 μM) treatment, cytotoxicity in U2OS and HOS cells had dose-dependent increases, and their half maximal inhibitory concentrations (IC50) of HO-3867 were 6.91 μM in U2OS cells, 7.60 μM in HOS cells, and 12.24 μM in MG-63 cells. Moreover, cell proliferation was assessed by using the CCK-8 method in U2OS and HOS cells. As shown in Figure 1C,D, treatment of cells with HO-3867 for 24 h significantly decreased the proportion of viable cells in a concentration-dependent manner. Reference: Pharmaceutics. 2022 Jun 13;14(6):1257. https://pubmed.ncbi.nlm.nih.gov/35745828/
In vivo activity:	This study further observed a significantly increased TUNEL-positive staining in tumor tissues treated with HO-3867, when compared to untreated controls (Fig 6D), suggesting that HO-3867 induced apoptosis in vivo. Quantitation of the TUNEL positive cells showed a fourfold increase after HO-3867 treatment in tumor mice as compared to the untreated control (Fig. 6E). The data supports the conclusion that HO-3867 inhibits endometrial cancer through targeting STAT3 and its targeting proteins of cell-cycle and apoptosis. Reference: Gynecol Oncol. 2014 Oct;135(1):133-41. https://pubmed.ncbi.nlm.nih.gov/25038288/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	20.0	43.05
	DMF:PBS (pH 7.2) (1:2)	0.3	0.71
	DMSO	18.3	39.46
	Ethanol	6.0	12.92

Preparing Stock Solutions

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:	1. Lu PW, Chou CH, Yang JS, Hsieh YH, Tsai MY, Lu KH, Yang SF. HO-3867 Induces Apoptosis via the JNK Signaling Pathway in Human Osteosarcoma Cells. Pharmaceutics. 2022 Jun 13;14(6):1257. doi: 10.3390/pharmaceutics14061257. PMID: 35745828; PMCID: PMC9229449. 2. Chen CW, Hsieh MJ, Ju PC, Hsieh YH, Su CW, Chen YL, Yang SF, Lin CW. Curcumin analog HO-3867 triggers apoptotic pathways through activating JNK1/2 signalling in human oral squamous cell carcinoma cells. J Cell Mol Med. 2022 Apr;26(8):2273-2284. doi: 10.1111/jcmm.17248. Epub 2022 Feb 21. PMID: 35191177; PMCID: PMC8995445. 3. Das A, Kamran M, Ali N. HO-3867 Induces ROS-Dependent Stress Response and Apoptotic Cell Death in Leishmania donovani. Front Cell Infect Microbiol. 2021 Dec 3;11:774899. doi: 10.3389/fcimb.2021.774899. PMID: 34926321; PMCID: PMC8677699. 4. Tierney BJ, McCann GA, Naidu S, Rath KS, Saini U, Wanner R, Kuppusamy P, Suarez A, Goodfellow PJ, Cohn DE, Selvendiran K. Aberrantly activated pSTAT3-Ser727 in human endometrial cancer is suppressed by HO-3867, a novel STAT3 inhibitor. Gynecol Oncol. 2014 Oct;135(1):133-41. doi: 10.1016/j.ygyno.2014.07.087. Epub 2014 Jul 16. PMID: 25038288; PMCID: PMC4283766.
In vitro protocol:	1. Lu PW, Chou CH, Yang JS, Hsieh YH, Tsai MY, Lu KH, Yang SF. HO-3867 Induces Apoptosis via the JNK Signaling Pathway in Human Osteosarcoma Cells. Pharmaceutics. 2022 Jun 13;14(6):1257. doi: 10.3390/pharmaceutics14061257. PMID: 35745828; PMCID: PMC9229449. 2. Chen CW, Hsieh MJ, Ju PC, Hsieh YH, Su CW, Chen YL, Yang SF, Lin CW. Curcumin analog HO-3867 triggers apoptotic pathways through activating JNK1/2 signalling in human oral squamous cell carcinoma cells. J Cell Mol Med. 2022 Apr;26(8):2273-2284. doi: 10.1111/jcmm.17248. Epub 2022 Feb 21. PMID: 35191177; PMCID: PMC8995445.
In vivo protocol:	1. Das A, Kamran M, Ali N. HO-3867 Induces ROS-Dependent Stress Response and Apoptotic Cell Death in Leishmania donovani. Front Cell Infect Microbiol. 2021 Dec 3;11:774899. doi: 10.3389/fcimb.2021.774899. PMID: 34926321; PMCID: PMC8677699. 2. Tierney BJ, McCann GA, Naidu S, Rath KS, Saini U, Wanner R, Kuppusamy P, Suarez A, Goodfellow PJ, Cohn DE, Selvendiran K. Aberrantly activated pSTAT3-Ser727 in human endometrial cancer is suppressed by HO-3867, a novel STAT3 inhibitor. Gynecol Oncol. 2014 Oct;135(1):133-41. doi: 10.1016/j.ygyno.2014.07.087. Epub 2014 Jul 16. PMID: 25038288; PMCID: PMC4283766.

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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, BognÃ¡r B, Khan M, KÃ¡lai 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, KÃ¡lai 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, KÃ¡lai 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, KÃ¡lai 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, KÃ¡lai 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, KÃ¡lai 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, KÃ¡lai 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, KÃ¡lai 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.

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