1. JAK/STAT Signaling
    Stem Cell/Wnt
    Apoptosis
  2. STAT
    Apoptosis
  3. STAT3-IN-10

STAT3-IN-10 

Cat. No.: HY-146728
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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.

For research use only. We do not sell to patients.

STAT3-IN-10 Chemical Structure

STAT3-IN-10 Chemical Structure

CAS No. : 2499491-04-0

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Description

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)

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].

MCE 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
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].

MCE 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.
Molecular Weight

311.29

Formula

C17H13NO5

CAS No.
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Storage

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STAT3-IN-10
Cat. No.:
HY-146728
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