STAT

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-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3).

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.

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

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 a Stat3 inhibitor with an IC50 of 4-7 μM.

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).

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin, Artesunate is soluble in water but has poor stability in aqueous solutions at neutral or acid pH.

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 (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.

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.

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].

Triacetylresveratrol (Acetyl-trans-resveratrol) has anti-cancer activity,it inhibits the phosphorylation of STAT3 and NFκB, down-regulates Mcl-1, and up-regulates Bim and Puma in pancreatic cancer cells.

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.