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STAT Signal transduction and activator of transcription

Cat.No.  Name Information
M3648 HO-3867 HO-3867, an analog of curcumin, is a selective STAT3 inhibitor.
M3982 Cryptotanshinone Cryptotanshinone is a potent anticancer agent targeting the activation STAT3 protein with antitumor activity.
M3970 Scutellarin Scutellarin, an active flavone isolated from Scutellaria baicalensis, is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively. Scutellarin inhibited caspase-11 activation and pyroptosis in macrophages at least partly via regulating the PKA signaling pathway.
M2883 Nifuroxazide Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells.
M2028 Fludarabine (NSC 118218) Fludarabine is a STAT1 activation inhibitor and a DNA synthesis inhibitor.
M3032 Stattic Stattic is the first nonpeptidic STAT3 inhibitor, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1. Stattic inhibits STAT3 phosphorylation (at Y705 and S727).
M7747 Diosgenin Diosgenin is a plant steroid which induces apoptosis in colon cancer cell lines and induces apoptosis, cell cycle arrest and COX activity in osteosarcoma cells.
M4433 Alantolactone Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone (helenin, helenine, Eupatal) could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.
M9706 Colivelin TFA Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3.
M10077 Colivelin Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3.
M30649 C188 C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).
M29919 inS3-54A18  inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.
M29859 UC-514321  UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
M29730 Ascochlorin 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.
M29716 Stafia-1  Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.
M29517 Pomstafib-2  Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis.
M29224 Stafib-2  Stafib-2 is a potent and selctive inhibitor of the transcription factor STAT5b, with an IC50 of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 exhibits poor cell permeability.
M28939 AC-4-130  AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).
M28810 Stafib-1  Stafib-1 is the first selective inhibitor of the STAT5b SH2 domain, with a Ki of 44 nM and an IC50 of 154 nM.
M28738 (S)-PM-43I  (S)-PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. (S)-PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research.
M28433 LY5  LY5 is a STAT3 inhibitor with an IC50 value of 0.5 μM. LY5 induces apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer.
M28215 IST5-002 IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML).
M28184 Debio 0617B  Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34+ stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors.
M27870 NSC-370284  NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5.
M27692 STAT3-IN-5  STAT3-IN-5 is a potent STAT3 inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC50 value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer.
M24985 Eflepedocokin alfa 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.
M22467 Danvatirsen Danvatirsen is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript.
M21406 SI-109 SI-109 is a potent STAT3 SH2 domain structural domain inhibitor (Ki=9 nM) with antitumor activity. si-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). si-109 and the CRBN analogue lenalidomide ligand were used to design the PROTAC STAT3 degradation agent SD- 36.
M20625 HJC0152 HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.




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