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STAT Signal transduction and activator of transcription

Inhibitors

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, a flavonoid glycoside, is the primary active ingredient in breviscapine that is a mixture of flavonoid glycosides extracted from a Chinese herb Erigeron breviscapus (Vant.) Hand.-Mazz.
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.
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.
M21381 AS1810722 AS1810722 is an orally effective STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows good CYP3A4 inhibition and is a thickened bicyclic pyrimidine derivative with potential for use in allergic disease studies, such as asthma and atopic diseases.
M20830 GYY4137 GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity.
M20625 HJC0152 HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
M14149 STAT3-IN-3 STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity.
M14148 STAT3-IN-1 STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
M11542 Ochromycinone Ochromycinone ((RAC-STA-21) is a natural antibiotic and a selective inhibitor of STAT3. Ochromycinone can inhibit STAT3 DNA binding activity and STAT3 dimerization. Ochromycinone has anticancer and antibacterial activities.
M10968 STAT5-IN-2 STAT5-IN-2 is an inhibitor of STAT5 in K562 and KU812 cells EC50 9 μM and 5 μM respectively, the name in Document 1 is 17f. STAT5-IN-2 has highly effective antileukemia activity.
M10697 Cucurbitacin I Cucurbitacin I is a naturally selective inhibitor of JAK2/STAT3 and has potent antitumor activity.
M10077 Colivelin Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3.
M9769 BP-1-102 BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor with IC50 of 6.8 μM.
M9706 Colivelin TFA Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3.
M9077 STAT5-IN-1 STAT5-IN-1 is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain, with an IC50 of 47 μM for STAT5β isoform.
M8874 C188-9 C188-9 is a small-molecule STAT3 inhibitor, can block Th2 and Th17 cell expansion and cytokine production to prevent house dust mite (HDM)-induced airway inflammation and remodeling.
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.
M7539 AS1517499 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.
M5264 SH5-07 SH5-07 is a robust hydroxamic acid-based STAT3 inhibitor, which induce antitumor cell effects in vitro and antitumor response in vivo against human glioma and breast cancer models.
M5018 Corylifol A Corylifol A is a phenolic compounds isolated from Psoralea corylifolia; inhibits IL-6-induced STAT3 activation and phosphorylation(IC50=0.8 uM).
M4622 Garcinone D Garcinone D is a natural xanthone from mangosteen, which increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3) in concentration- and time- dependent manners.
M4493 Casticin (Vitexicarpin) Casticin (Vitexicarpin) is a methoxyl flavonoid compound obtained from fructus vitae and has anti-mitotic and anti-inflammatory activities. Casticin inhibits the activation of STAT3.



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