ζ-stat

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.

Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3 Girdin Akt signaling in HCC cells.

C188-9 (TTI-101) is a Stat3 inhibitor with an IC50 of 4-7 μM.

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.

Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].

Niclosamide (Niclocide)(BAY2353) is used to treat most tapeworm infections by inhibiting DNA replication.

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.

SD-36 is a selective and efficient STAT3 protein degrader (Kd=~50 nM) with antitumor activity that promotes growth inhibition and induces apoptosis by inhibiting Mcl-1 in gliomas.SD-36 inhibits the transcriptional activity of STAT3.

STX-0119 is a selective, orally active STAT3 dimerization inhibitor that suppresses STAT3 transcription with an IC50 of 74 μM.

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines.

HJC0152 hydrochloride (HJC0152) is a signal transducer and activator of transcription 3 (STAT3) inhibitor.

Ochromycinone (STA 21) is a selective STAT3 inhibitor.

Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2 STAT3 with anti-cancer activity.

1. Morusin (Mulberrochromene) possesses antitumor effects of cell lines including HT-29, A549, MCF-7, and MDA-MB-231, through suppressing STAT3 and NFκB attenuation mediated apoptosis induction. 2. Morusin possesses anti-oxidant and anti-inflammatory effects.

AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Homoharringtonine (HHT) is a natural alkaloid that inhibits the translation of proteins and is cytotoxic. Homoharringtonine acts on the ribosomes of tumor cells to inhibit the elongation step of protein translation, thereby inhibiting protein synthesis, and has antitumor activity.

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

W1131 TFA is a potent STAT3 inhibitor inducing ferroptosis and effectively halting cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. It mitigates chemoresistance to 5-FU in cancer cells and modulates the cell cycle, DNA damage response, and oxidative phosphorylation, targeting pathways such as IL6-JAK-STAT3 and ferroptosis [1].

Neocucurbitacin A (compound 7), a STAT3 inhibitor extracted from the pericarp of Aquilaria crassna, serves as a potential agent for anticancer research [1].

JI069 (WAY-354189) is a potent STAT3 inhibitor that inhibits gp130 signaling by inducing dissociation between gp130 and JAK1.

iBFAR2, an inhibitor of BFAR, restores the CD8+ tumor-resident memory T cell subset against solid tumors. It promotes the binding of JAK2-STAT1 and enhances the phosphorylation of STAT1.

AJI-214 functions as a dual-target inhibitor that specifically blocks Aurora kinase A and JAK2. By directly inhibiting Aurora kinase A, AJI-214 prevents mitotic progression and cell polarity in T cells while concurrently suppressing JAK2 activation to reduce STAT3 phosphorylation. This inhibition decreases the differentiation of TH1 and TH17 cells. AJI-214 is utilized in research focused on the modulation of immune responses and the prevention of graft-versus-host disease (GVHD).