2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. HJC0416

HJC0416 是一种有效的口服活性 STAT3 抑制剂 HJC0416 显示出抗增殖活性并诱导细胞凋亡 (apoptosis). HJC0416 降低 p-STAT3 (Tyr-705)、Cyclin D1 的表达并增加cleaved caspase-3 蛋白的表达。HJC0416 显示出抗肿瘤活性。

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HJC0416 Chemical Structure

HJC0416 Chemical Structure

CAS No. : 1617518-22-5

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HJC0416 的其他形式现货产品:

Customer Review

Other Forms of HJC0416:

HJC0416 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity[1].

IC50 & Target[1]

STAT3

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
ASPC1 IC50
0.04 μM
Compound: 12, HJC0416
Antiproliferative activity against human AsPC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
Antiproliferative activity against human AsPC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
[PMID: 24904966]
MCF7 IC50
1.76 μM
Compound: 12, HJC0416
Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
[PMID: 24904966]
MDA-MB-231 IC50
1.97 μM
Compound: 12, HJC0416
Antiproliferative activity against ER-negative and triple-negative human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
Antiproliferative activity against ER-negative and triple-negative human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
[PMID: 24904966]
PANC-1 IC50
1.88 μM
Compound: 12, HJC0416
Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
[PMID: 24904966]
体外研究
(In Vitro)

HJC0416 (0-10 µM; 48 h) 在 MDA-MB-231 细胞中显示抗增殖活性并诱导细胞凋亡[1]。
HJC0416 (0-10 µM; 12 h) 降低 p-STAT3 (Tyr-705)、Cyclin D1 的表达并增加cleaved caspase-3 蛋白的表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HJC0416 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231, AsPC1, Panc-1 cells
Concentration: 0-100 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s 1.76, 1.97, 0.04, 1.88 µM for MCF-7, MDA-MB-231, AsPC1, Panc-1 cells, respectively.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 5, 10 µM
Incubation Time: 48 h
Result: Induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 1, 5, 10 µM
Incubation Time: 12 h
Result: Suppressed the expression of phosphorylated STAT3 at Tyr-705, Cyclin D1, increased the expression of cleaved caspase-3.
体内研究
(In Vivo)

HJC0416 (腹腔注射 10 mg/kg；口服 100 mg/kg；每日一次，持续 7 天) 在小鼠中减少肿瘤生长，体重没有明显减轻[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6 weeks, female nude mice (MDA-MB-231 cells)[1]
Dosage: 10 mg/kg for i.p.; 100 mg/kg for p.o.
Administration: I.p. or p.o.; daily for 7 days
Result: Decreased the tumor volume for 67% as compared to the control mice for i.p.; the growth of xenograft tumors in mice was also significantly reduced at a dose of 100 mg/kg by 46%.
分子量

392.86

Formula

C18H17ClN2O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HJC0416 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HJC04161617518-22-5HJC 0416HJC-0416STATApoptosisantiprolifeativeantitumororally activeapoptosisMDA-MB-231 cellsp-STAT3 (Tyr-705)Cyclin D1cleaved caspase-3Inhibitorinhibitorinhibit

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