STAT3-IN-10

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

STAT3-IN-10 

STAT3-IN-10 (A11) 是一个 IC50 值为5.18 µM 的 STAT3 抑制剂。STAT3-IN-10 与 STAT3 SH2 结构域直接结合,抑制肿瘤细胞生长和诱导肿瘤细胞的凋亡 (apoptosis)

STAT3-IN-10

STAT3-IN-10 Chemical Structure

CAS No. : 2499491-04-0

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生物活性

STAT3-IN-10 (A11) is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells[1].

IC50 & Target

STAT3

5.18 μM (IC50)

体外研究
(In Vitro)

STAT3-IN-10 (A11) (48 h) shows IC50 values of 0.67, 0.77, 1.24 µM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively[1].
STAT3-IN-10 (A11) directly binds to the STAT3 SH2 domain [1].
STAT3-IN-10 (A11) (0-3 μM, 24 h) inhibits the phosphorylation of STAT3 and its downstream target proteins and has a good selectivity against the tumor suppressor STAT1 [1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) induces apoptosis in cancer cells[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) dose-dependently causes a significant S phase arrest in MDA-MB-231 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2.
Concentration:
Incubation Time: 48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2).
Result: Showed IC50 values of 0.67, 0.77, 1.24 µM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231.
Concentration: 0, 0.75, 1.5 and 3.0 μM.
Incubation Time: 24 h.
Result: Decreased the STAT3-Y705 phosphorylation without affecting the total amount of STAT3 protein and decreased the expression of STAT3 target genes, including C-Myc and Cyclin D1 in a dose-dependent manner. Had little impact on the level of STAT1 and its phosphorylation on Tyr701.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231.
Concentration: 0, 1, 2, and 4 μM.
Incubation Time: 24 h.
Result: Induced the apoptosis in MDA-MB-231 cells in a concentration-dependent manner

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231.
Concentration: 0, 1, 2, and 4 μM.
Incubation Time: 24 h.
Result: Could dose-dependently cause a significant S phase arrest in MDA-MB-231 cells

体内研究
(In Vivo)

STAT3-IN-10 (A11) (5 and 10 mg/kg; IP; once a day, 21 days) inhibits the growth of human xenograft tumor in vivo[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five weeks old female BALB/c nude mice (16–18g) bearing inoculation of human breast cancer cells MDA-MB-231[1].
Dosage: 5 and 10 mg/kg
Administration: IP, once a day, 21 days
Result: Inhibited the growth of human xenograft tumor in vivo without apparent body-weight loss for treated mice and inhibited the levels of p-STAT3 in tumor tissues.

分子量

311.29

Formula

C17H13NO5

CAS 号

2499491-04-0

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.

参考文献
  • [1]. Kai-Rui Feng, et al. Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy. Eur J Med Chem. 2020 Sep 1;201:112428.

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