STAT3-IN-3

STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.

Product information

CAS Number: 2361304-26-7

Molecular Weight: 600.48

Formula: C27H26BrN3O6S

Chemical Name: 4-bromo-2-{4-[7-(diethylamino)-2-oxo-2H-chromene-3-carbonyl]piperazine-1-carbonyl}-1-benzothiophene-1, 1-dione

Smiles: CCN(CC)C1=CC2OC(=O)C(=CC=2C=C1)C(=O)N1CCN(CC1)C(=O)C1=CC2=C(Br)C=CC=C2S1(=O)=O

InChiKey: LEVMMUZFAXTJOJ-UHFFFAOYSA-N

InChi: InChI=1S/C27H26BrN3O6S/c1-3-29(4-2)18-9-8-17-14-20(27(34)37-22(17)15-18)25(32)30-10-12-31(13-11-30)26(33)24-16-19-21(28)6-5-7-23(19)38(24,35)36/h5-9,14-16H,3-4,10-13H2,1-2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 5 mg/mL (8.33 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

STAT3-IN-3 has no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2. STAT3-IN-3 inhibits the growth of MDA-MB-231, HCT-116, HepG2, and MCF-7 cells with IC50s of 1.43 μM, 1.89 μM, 2.88 μM, and 3.33 μM, respectively. STAT3-IN-3 down-regulates the expression of STAT3 target genes Bcl-2 and Cyclin D1. STAT3-IN-3 inhibits STAT3 tyrosine phosphorylation and serine phosphorylation. STAT3-IN-3 inhibits STAT3 DNA-binding activity. STAT3-IN-3 (1-4 μM; 24 hours) increases ROS production and remarkably reduces the mitochondrial membrane potential to induce mitochondrial apoptotic pathway. STAT3-IN-3 (1-4 μM; 24 hours) can induce the cleavage of caspase-9, caspase-3 and PARP.

In Vivo:

STAT3-IN-3 (10mg/kg-20 mg/kg; i.p.; daily; for 14 days) possesses potent antitumor activity against implanted 4T1 breast tumors growth.

References:

1. Cai G, et al. Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors. Eur J Med Chem. 2019 Jul 15;174:236-251.

Products are for research use only. Not for human use.