stat3-in-1

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.

JAK2 STAT3-IN-1 is a GP130 inhibitor with anti-tumor effects and can be used to study inflammation, autoimmunity and cancer.

JAK1 STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1 STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1 STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1 JAK1 and p-STAT3 STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).

(R)-JAK2 STAT3-IN-10a is the R-isomer of JAK2 STAT3-IN-1.JAK2 STAT3-IN-1 is a GP130 D1 structural domain inhibitor with antitumor activity that inhibits the phosphorylation of JAK2 and STAT3. The KD value of (R)-JAK2 STAT3-IN-1 on GP130 protein is 3.8 μM.

STAT3-IN-10 (A11) is an inhibitor of STAT3 that directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells (IC 50 = 5.18 μM) [1].

STAT3-IN-14 is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 can directly bind to the hinge region of STAT3 .

Row174336 (compound 29) serves as an efficient inhibitor of the Hsp110-STAT3 interaction, exhibiting antiproliferative activity in the HPAEC cell line with an IC50 of 22.67 μM.

STAT3-IN-11 is a selective STAT3 inhibitor with inhibitory effects on phosphorylation of the STAT3pTyr705 site and phosphorylation of Survivin.STAT3-IN-11 promotes apoptosis in cancer cells and is a candidate compound for the treatment of cancer.

STAT3-IN-13 is a potent STAT3 inhibitor.STAT3-IN-13 has antiproliferative and anticancer activity and acts by binding to the structural domain of STAT3 SH2.STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705, which induces apoptosis and inhibits tumor cell growth and metastasis.STAT3-IN-13 can be used to study breast cancer and liver cancer. The study of breast cancer and hepatocellular carcinoma.

STAT3-IN-12 is a potent inhibitor of STAT3 signaling, effectively inhibiting IL-6-induced activation of the JAK STAT3 pathway. It suppresses cancer cell growth and migration, blocks the cell cycle, and induces apoptosis in HCC and oesophageal cancer.

STAT3-IN-15, a potent and orally active inhibitor targeting STAT3, effectively combats idiopathic pulmonary fibrosis (IPF) by hindering STAT3 phosphorylation. Additionally, it impedes TGF-β1-induced migration and deformation of epithelial cells and prevents epithelial-mesenchymal transition (EMT), offering a multifaceted approach against IPF.

STAT3-IN-18 (compound SPP), a platinum (IV) complex featuring an axial ligand from sandalwood, suppresses the JAK2-STAT3 pathway in breast cancer (BC) cells and exhibits anti-proliferative properties. It promotes apoptosis by activating caspase-3 and elevating levels of cleaved polyADP-ribose polymerase, in addition to enhancing maturation and antigen presentation in dendritic cells. Moreover, STAT3-IN-18 has demonstrated in vivo safety.

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].

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.

SD-36 TFA is a selective and highly efficient STAT3 degrader with a Kd value of about 50 nM.SD-36 has anticancer and antitumor activity, and can break down mutant STAT3 proteins in cells and inhibit STAT3 transcription.SD-36 promotes growth inhibition and induces apoptosis through inhibition of Mcl-1 in gliomas.

SC-2001 is a MCL-1 inhibitor. SC-2001 inhibits STAT3 phosphorylation through enhancing SHP-1 expression and induces apoptosis in human breast cancer cells. SC-2001 overcomes STAT3-mediated sorafenib resistance through RFX-1 SHP-1 activation in hepatocellu

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.

Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.

BP-1-102 is an orally active, effective, and specific STAT3 inhibitor that binds Stat3 (Kd: 504 nM), blocks Stat3-phosphotyrosine (pTyr) peptide interactions and Stat3 activation (4-6.8 μM), and selectively inhibits the migration, survival, growth, and invasion of Stat3-dependent tumor cells. The BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of [c-Myc, Bcl-xL, Cyclin D1, Survivin, and VEGF].

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

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin that inhibits cyclooxygenase. It induces cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells by down-regulating EGFR PI3K STAT3 signaling and modulating Bcl-2 family proteins. Additionally, Nitroaspirin possesses antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.