JAK-STAT-IN-1 (compound 1) is a selective JAK-STAT inhibitor. JAK-STAT-IN-1 can be used for the research of autoimmune disorder[1].
15-keto-Prostaglandin E2 is an endogenous metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to its Cys259 residue. 15-keto-Prostaglandin E2 can bind and stabilize EP2 and EP4 receptor. 15-keto-Prostaglandin E2 inhibits breast cancer cell growth and progression. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth[1][2][3].
Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of human platelets in mouse xenotransplantation assay[1].
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3].
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity[1][2][3].
Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells[1].
A potent, selective STAT3 inhibitor that blocks STAT3 binding to its phosphopeptide ligand (IC50=20 uM) and inhibits IL-6-mediated phosphorylation of STAT3; inhibits nuclear translocation of phosphorylated Stat3 with IC50 of 39 uM, induces apoptosis preferentially of breast cancer cell lines with constitutive Stat3 activation.
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation[1].
Eflepedocokin alfa is a recombinant fusion protein with potential cell protective activity. Eflepedocokin alfa consists of human IL-22 fused to human IgG2-Fc domain. Eflepedocokin alfa leads to the activation of IL-22/IL-22R-mediated signal transduction pathways as well as STAT3. Eflepedocokin alfa plays a role in immune response and bacterial infection, enhancing intestinal barrier function, intestinal immunity, and tissue repair[1].
Neocucurbitacin A (compound 7) is STAT3 inhibitor a compound extracted from Aquilaria crassna pericarp. Neocucurbitacin A can be used for anticancer research[1].
STAT6-IN-3 (Compound 18a) is a STAT6 inhibitor (IC50= 44 nM). STAT6-IN-3 targets the Src Homology 2 (SH2) domain of STAT6. STAT6-IN-3 can be used for research of inflammation such as asthma[1].
Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners[1].
Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects[1].
Eucannabinolide is a STAT3 inhibitor. Eucannabinolide suppresses STAT3 activation at tyrosine 705, inhibiteds its translocation to nucleus, and decreases its DNA binding capacity. Eucannabinolide can be used for triple negative breast cancer (TNBC) diseases research[1].
Niclosamide-13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate[1]. Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research[2]. Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells[5]. Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells[3][4][6].
Tetramethylcurcumin (FLLL31), derived from curcumin, specifically suppresses the phosphorylation of STAT3 by binding selectively to Janus kinase 2 and the STAT3 Src homology-2 domain. Tetramethylcurcumin exhibits anti-inflammatory and anti-cancer effects[1][2].
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon[1].
(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1].
Balsalazide-d4 is deuterium labeled Balsalazide. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
NT219 is a potent and dual inhibitor of insulin receptor substrates 1/2 (IRS1/2) and STAT3. IRS1/2 and STAT3 are major signaling junctions regulated by various oncogenes. NT219 affects IRS1/2 degradation and inhibits STAT3 phosphorylation. NT219 has the potential for the research of cancer diseases[1].
UC-514321 is a more effective analog of NSC-370284 that directly binds to STAT3/5, significantly and selectively suppresses the viability of AML cells with high level of TET1 expression both in vitro and in vivo; shows no inhibitory effect on the viability of TET1-low AML (i.e., NB4) cells, function as TET1-transcription inhibitor in TET1-high AMLs and the anti-leukemic effects are TET1-dependent.
L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM. L002 has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 µM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases[1]. L002 blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation[2].
Artesunate-d4 is deuterium labeled Artesunate. Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
STAT3-IN-20 (Compound 40) is a selective STAT3 inhibitor (IC50: 0.65 μM). STAT3-IN-20 binds the SH2 domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC50: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis[1].
C188-9 is a Stat3 inhibitor, with a Kd of 4.7 nM.
STAT3-IN-23 (PY*LKTK) is a potent STAT3 inhibitor[1].
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis[1].
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1][2].