HO-3867 selectively inhibits the phosphorylation and transcription of STAT3. It is an analog of curcumin.
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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。 |
靶点 |
|
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] |
Dose | Mice: 20 mg/kg[3] (i.v.) Rat: 10 mg/kg, 25 mg/kg[4] (i.p.) |
Administration | i.v., i.p. |
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 |
CAS号 | 1172133-28-6 |
分子式 | C28H30F2N2O2 |
分子量 | 464.55 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
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 |