STAT

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.

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.

STAT5-IN-2 is an inhibitor of STAT5 with antileukemic effects (EC50s: 9 μM and 5 μM in K562 and KU812 cells, respectively).

STAT5-IN-1 (STAT5 Inhibitor) is a cell-permeable inhibitor which suppresses Stat5 via binding to the SH2 domain.

STAT3-IN-3 is a potent and highly selective targeted STAT3 inhibitor with significant anti-proliferative activity. It effectively induces apoptosis in breast cancer cells. As a mitochondrially targeted STAT3 inhibitor with great research potential, it has good application value in tumor mechanism exploration and anti-cancer research.

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.

ζ-Stat (NSC37044), a specific and atypical inhibitor of PKC-ζ with an IC50 of 5 μM, demonstrates the ability to inhibit proliferation and induce apoptosis in melanoma cell lines, exhibiting antitumor activity in vitro[1][2].

ζ-Stat trisodium (NSC37044 trisodium) is a potent and selective inhibitor of protein kinase C-ζ (PKC-ζ) with an IC50 of 5 μM. It effectively suppresses melanoma cell proliferation, induces apoptosis, and shows significant in vitro antitumor activity.

Niclosamide is a classic salicylanilide antiparasitic drug and a multi-target, low-toxicity, broad-spectrum small-molecule modulator with anthelmintic and antitumor activity. Niclosamide disrupts the parasite’s energy metabolism by uncoupling mitochondrial oxidative phosphorylation, leading to reduced ATP production and ultimately killing the parasite. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

2-NP is a STAT1 enhancer.

C188-9 (TTI-101) is an orally administered, highly selective STAT3 SH2 domain inhibitor with a Kd value of 4.7 nM. C188-9 induces apoptosis in AML cell lines and primary samples while inhibiting colony formation in primary AML cells. C188-9 is suitable for studies on tumors, inflammation, and immune evasion.

Colivelin is a neuroprotective peptide and activator of STAT3. Colivelin is a hybrid peptide synthesized to enhance the neuroprotective effects of humanin (HN).

(R)-Lisofylline ((R)-Lisophylline) is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 µM) that interrupts IL-12 signaling-mediated STAT4 activation, making it useful for studies on the treatment of type 1 diabetes and autoimmune disorders.

FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).

Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.

Artesunate (WR-256283) is a semisynthetic derivative of artemisinin and an inhibitor of STAT-3/EXP1. Water-soluble yet relatively unstable in neutral or acidic aqueous solutions, Artesunate is primarily employed for the treatment of malaria.

Niclosamide olamine (Niclosamide Ethanolamine salt) is an Repellent, Insect Attractant and Chemosterilant.

Nifuroxazide (Diarlidan) is an orally available and cell-permeable nitrofuran-based antidiarrheal agent. It has the inhibitory effect against the activation of cellular STAT1/3/5 transcription.

Scutellarin (Breviscapin) is a natural flavonoid isolated from Scutellaria baicalensis that exhibits antioxidant, anti-inflammatory, antithrombotic, neuroprotective, and cardioprotective and neuroprotective activities. Scutellarin demonstrates antiviral activity against HIV-1 IIIB, HIV-1 (74V), and HIV-1 KM018. Scutellarin inhibits the RANKL-mediated MAPK/NF-κB pathway (IC₅₀ = 10 μM) and activates the Nrf2/HO-1 antioxidant pathway (EC₅₀ = 5 μM). Scutellarin can be used in natural product development and basic research on cardiovascular and cerebrovascular diseases.

Cryptotanshinone (Cryptotanshinon), a STAT3 inhibitor (IC50: 4.6 μM) in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a little effect on STAT3 Ser727, but no inhibition for STAT1 nor STAT5.

Diosgenin (Nitogenin) is a spirostan found in DIOSCOREA and other plants. It has favorable effects in the improvement of diabetes and regulation of lipid metabolism.

Alantolactone is a selective inhibitor of STAT3 that induces cancer-associated apoptosis and has antitumor activity.