stat3 in mda-mb 231 cells

STAT3-IN-1 selective and orally active inhibitor of STAT3(in HT29 and MDA-MB 231 cells, with IC50 values of 1.82 μM and 2.14 μM , respectively), induces tumor apoptosis.

STAT3-IN-B9 (B9) is an inhibitor of abnormal STAT3 activation and inhibits the proliferation of tumor cells including MDA-MB-468, MDA-MB-231, and DU145.

PMMB-187, a selective STAT3 inhibitor, exhibits an IC50 of 1.81 μM in MDA-MB-231 cells. This compound induces apoptosis in MDA-MB-231 cells by inhibiting STAT3 transcriptional activity and nuclear translocation, reducing mitochondrial membrane potential, increasing reactive oxygen species (ROS) production, and upregulating the expression of apoptosis-related proteins. PMMB-187 is useful for research in the field of cancer.

WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).

Antitumor agent-195 (compound 16c) is a dual-targeting agent that simultaneously targets STAT3 and NQO1. At a concentration of 1 μM, it significantly inhibits the phosphorylation of STAT3 at the Tyr705 site and effectively induces apoptosis in MDA-MB-231 and MDA-MB-468 breast cancer cells. As a substrate of NQO1, Antitumor agent-195 markedly increases ROS production, causing severe DNA damage in a dose-dependent manner. It also demonstrates strong antitumor properties in MDA-MB-231 xenograft models.

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). It induces ferroptosis by elevating reactive oxygen species (ROS) and lipid peroxides. This compound also inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 is applicable for research in triple-negative breast cancer (TNBC).

STAT3-IN-52 (Compound 9) is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3). It binds to the pY705 site of STAT3 with a Ki of 440 nM, effectively hindering STAT3 phosphorylation and dimerization. STAT3-IN-52 exhibits potent cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 of 0.7 μM), medulloblastoma UW426, and pancreatic cancer BKPC3 cells. The compound induces apoptosis, inhibits STAT3's nuclear translocation and DNA-binding activity, and downregulates the expression of the STAT3 target gene MMP9. STAT3-IN-52 is useful in research related to cancers with aberrant STAT3 activation.

Axl-IN-21 is an orally bioavailable selective AXL inhibitor with a Kd of 2.7 nM and an IC50 of 4.0 nM. It demonstrates strong inhibitory activity against various cancer-related kinases while maintaining kinase selectivity, including Mer (Kd = 1.4 nM), DDR1 (IC50 = 22.2 nM), HIPK4 (Kd = 11.0 nM), and LOK (Kd = 10 nM). By blocking the AXL/STAT3/ABCG1 signaling pathway induced by GAS6 from tumor-associated fibroblasts, Axl-IN-21 can overcome tumor microenvironment-driven resistance, restore chemotherapy sensitivity, and inhibit drug efflux. In MDA-MB-231 cells, it inhibits TGF-β1-induced epithelial-mesenchymal transition, cell migration, and invasion. Axl-IN-21 exhibits no significant toxicity to non-cancer cells and is relevant for research in triple-negative breast cancer and gastric cancer.

STAT3-IN-49 (compound B16) is a potent and selective inhibitor of STAT3. It binds to the SH2 domain of STAT3, blocking its phosphorylation and nuclear translocation. STAT3-IN-49 inhibits migration, invasion, and colony formation in triple-negative breast cancer (TNBC) cells. Additionally, it suppresses tumor growth in the MDA-MB-231 xenograft mouse model. STAT3-IN-49 is applicable for TNBC research.

STAT3-IN-33 (compound 7f) is a potent STAT3 inhibitor with anticancer properties. It exhibits antiproliferative activity in HCT116, MCF-7, and MDA-MB-231 cells, with IC50 values of 6.44, 3.29, and 4.86 μM, respectively. STAT3-IN-33 is applicable for breast and colon cancer research.

Downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, HJC-0123 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.

Nifuroxazide-D4 is intended for use as an internal standard for the quantification of nifuroxazide by GC- or LC-MS. Nifuroxazide (T1563) is a nitrofuran antibiotic. It is active against strains of the enteropathogenic bacteria C. jejuni, Salmonella, Y. enterocolitica, Shigella, and E. coli. It inhibits quorum sensing and virulence factor production in P. aeruginosa. Nifuroxazide (T1563) inhibits STAT3 activity in a reporter assay and decreases viability of U266 and INA-6 myeloma cells, which have constitutive STAT3 phosphorylation, with EC50 values of approximately 4.5 µM for both. It also decreases viability, migration, and invasion of, and induces apoptosis in, MCF-7, 4T1, and MDA-MB-231 breast cancer cells. Nifuroxazide (T1563) reduces tumor growth and prevents pulmonary metastasis in a 4T1 murine mammary carcinoma model. It also reduces diarrhea, weight loss, and colon inflammation in a rat model of acetic acid-induced ulcerative colitis.

JMX0293, an O-alkylamino-tethered salicylamide derivative, demonstrates strong efficacy against the TNBC MDA-MB-231 cell line with an IC50 of 3.38 μM, while showing minimal toxicity towards the non-tumorigenic human breast epithelial cell line MCF-10A, where its IC50 exceeds 60 μM. It inhibits STAT3 phosphorylation, contributing to apoptosis in MDA-MB-231 cells, and significantly suppresses MDA-MB-231 xenograft tumor growth in vivo, all without notable toxicity.

Erasin is a STAT3 inhibitor (IC50 = 9.7 μM) with higher selectivity for inhibiting STAT3 tyrosine phosphorylation than STAT5 and STAT1. It induces apoptosis in various cancer cell lines (e.g., MDA-MB-231, HCC-827) and is effective against Erlotinib-resistant cancer cells.

SBT-100 is a human monoclonal antibody (mAb) that targets STAT3. It inhibits IL-6-mediated nuclear translocation of P-STAT3 in HEp-2 and PANC-1 cells and demonstrates tumor growth inhibition in MDA-MB-231.