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HO-3867 97%

货号:A909125 Ambeed 开学季,买赠积分,赢豪礼

HO-3867 selectively inhibits the phosphorylation and transcription of STAT3. It is an analog of curcumin.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
HO-3867 化学结构 CAS号:1172133-28-6
HO-3867 化学结构
CAS号:1172133-28-6
HO-3867 3D分子结构
CAS号:1172133-28-6
HO-3867 化学结构 CAS号:1172133-28-6
HO-3867 3D分子结构 CAS号:1172133-28-6
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HO-3867 纯度/质量文件 产品仅供科研

货号:A909125 标准纯度: 97%
批次查询: 批次纯度:

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产品名称 STAT1 STAT3 STAT5 其他靶点 纯度
Nifuroxazide 98%
Fludarabine 98%
Artesunate 98%
BP-1-102 +++

STAT3, Kd: 504 nM

99%+
Niclosamide ++

STAT3, IC50: 0.7 μM

98%
Napabucasin 98%
Cryptotanshinone ++

STAT3, IC50: 4.6 μM

98%
Stattic +

STAT3, IC50: 5.1 μM

98%
NSC 74859 +

STAT3, IC50: 86 μM

99%+
Ochromycinone 98%
HO-3867 97%
C188-9 ++++

STAT3, Kd: 4.7 nM

99%+
HJC0152 98%
SH5-07 97%
SH-4-54 ++++

STAT3, Kd: 300 nM

+++

STAT5, Kd: 464 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

HO-3867 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]

HO-3867 动物研究

Dose Mice: 20 mg/kg[3] (i.v.) Rat: 10 mg/kg, 25 mg/kg[4] (i.p.)
Administration i.v., i.p.

HO-3867 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.

HO-3867 实验方案

计算器
存储液制备 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

HO-3867 技术信息

CAS号1172133-28-6
分子式C28H30F2N2O2
分子量 464.55
别名
运输蓝冰
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
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