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HO-3867

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Chemical Structure| 1172133-28-6 同义名 : -
CAS号 : 1172133-28-6
货号 : A909125
分子式 : C28H30F2N2O2
纯度 : 97%
分子量 : 464.55
MDL号 : MFCD28143913
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(64.58 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • STAT3
描述 HO-3867, a curcumin analogue, is a selective STAT3 inhibitor. It selectively inhibited STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs at 10μM. HO-3867 significantly inhibited BRCA-mutated ovarian cancer cells expressing higher level of Tyrosine-phosphorylated STAT3 (pTyr705) in vitro, in a dose (1-20μM)- and time (12-48h)-dependent manner, with apoptosis shown by elevated levels of cleaved caspase-3, caspase-7 and PARP. Also, treatment with HO-3867 resulted in decreased expression of pTyr705 and its downstream targets cyclin D1, Bcl-2 and surviving in these cells. HO-3867 is a safe STAT3 Inhibitor for it exhibited minimal toxicity toward noncancerous cells and tissues but induced apoptosis in ovarian cancer cells. It inhibited cell migration/invasion and survival of primary human ovarian cancer cells isolated from patient ascites at 10μM post 24h. Administration of HO-3867 at 100ppm could block xenograft tumor growth without toxic side effects in nude mice injected with A2780 cells.
作用机制 HO-3867 has high affinity for a pocket located on the DNA-binding domain of the STAT3 and it could interact with both the STAT3 dimer and monomer structures.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.53mL

4.31mL

2.15mL
参考文献

[1]Rath KS, Naidu SK, et al. HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27.

[2]Tierney BJ, McCann GA, et al. 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.

[3]Madan E, Parker TM, et al. The curcumin analog HO-3867 selectively kills cancer cells by converting mutant p53 protein to transcriptionally active wildtype p53. J Biol Chem. 2018 Mar 23;293(12):4262-4276.

[4]Dayton A, Selvendiran K, et al. 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.