STAT3-IN-11_product_DataBase

Bioactivity

STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers[1].

Target

IC50: 1.93 μM (SIP), ≥ 30 μM (SphK1), ≈ 30 μM (SphK2).

Invitro

STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells[1].STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-1) [1].STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the phosphorylation of STAT3 (stimulated by IL-6 in MDA-MB-231) at site pTyr705 in a dose-dependent manner[1].STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the expression of the downstream gene (Survivin and Mcl-1) of STAT3 in a concentration-dependent manner[1].STAT3-IN-11 (2.5-10 μM, 6 h) has no effects on the typical upstream kinases of STAT3 such as p-JAK2 and p-Src and the phosphorylation of STAT1 (a STAT isoform) [1].STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner[1]. Cell Cytotoxicity Assay[1] Cell Line:

Name

STAT3-IN-11

CAS

2503096-50-0

Formula

C20H17NO4

Molar Mass

335.35

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Li N, et al. Design, synthesis and biological evaluation of novel plumbagin derivatives as potent antitumor agents with STAT3 inhibition. Bioorg Chem. 2020 Nov;104:104208.

PeptideDB

STAT3-IN-11

CAS: 2503096-50-0 F: C20H17NO4 W: 335.35