STAT3-IN-11 

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].

IC₅₀: 1.93 μM (SIP), ≥ 30 μM (SphK1), ≈ 30 μM (SphK2)^[1].

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].

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

335.35

Solid

C₂₀H₁₇NO₄

2503096-50-0

O=C(NCCC(C1=O)=C(C)C(C2=C1C(O)=CC=C2)=O)C3=CC=CC=C3

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]