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STAT

The JAK-STAT signalling pathway is a chain of interactions between proteins in a cell, and is involved in processes such as immunity, cell division, cell death and tumour formation. There are 4 JAK proteins: JAK1, JAK2, JAK3 and TYK2. JAKs contains a FERM domain (approximately 400 residues), an SH2-related domain (approximately 100 residues), a kinase domain (approximately 250 residues) and a pseudokinase domain (approximately 300 residues). The kinase domain is vital for JAK activity, since it allows JAKs to phosphorylate (add phosphate groups to) proteins.

  • AS2863619
    T83782241300-51-4
    AS2863619 is an orally active inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).
    • $133
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  • Kurarinone
    T5S099334981-26-5
    Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflammatory skin diseases through the suppression of pathogenic CD4(+) T-cell differentiation and the overall immune response.
    • $39
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  • Alantolactone
    T2896546-43-0
    Alantolactone (Inula camphor)(Alant camphor), a sesquiterpene lactone, has potential activity against triple-negative breast Y MDA-MB-231 cells by suppressing the signal transducer and activator of transcription 3 (STAT3) signaling pathway.
    • $50
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  • Cucurbitacin I
    TQ01962222-07-3
    Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
    • $78
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  • Triacetylresveratrol
    T566842206-94-0
    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.
    • $68
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  • Nifuroxazide
    T1563965-52-6
    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.
    • $38
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  • Ginkgetin
    T4S2126481-46-9
    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
    • $120
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  • JI069
    T77672850019-35-1
    JI069 (WAY-354189) is a potent STAT3 inhibitor that inhibits gp130 signaling by inducing dissociation between gp130 and JAK1.
    • $195
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  • inS3-54-A26
    T27613328998-77-2In house
    inS3-54-A26 is an inhibitor of the DNA-binding domain of STAT3. inS3-54-A26 suppresses tumor growth, metastasis and the gene expression of STAT3.
    • $117
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  • MMPP
    T280771895957-18-2In house
    MMPP is a novel VEGFR2 inhibitor with anti-inflammatory and potential anticancer activity, inhibits STAT3, inhibits angiogenesis via VEGFR2/AKT/ERK/NF-kappaB pathway, and can be used to alleviate myocardial injury.
    • $257
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  • JAK-STAT-IN-1
    T786071236666-76-4In house
    JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.
    • $195 TargetMol
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  • STAT3-IN-B9
    T28865825611-06-1In house
    STAT3-IN-B9 (B9) is an inhibitor of abnormal STAT3 activation and inhibits the proliferation of tumor cells including MDA-MB-468, MDA-MB-231, and DU145.
    • $195
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  • ML116
    T8597744270-00-6
    ML116 is a potent and selective STAT3 inhibitor.
    • $133
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  • (R)-Lisofylline
    T21694100324-81-0In house
    (R)-Lisofylline ((R)-Lisophylline) is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 µM). (R)-Lisofylline interrupts IL-12 signaling-mediated STAT4 activation and can be used in studies about the treatment of type 1 diabetes and autoimmune disorders.
    • $227
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  • Cenisertib
    T14925871357-89-0In house
    Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.
    • $987
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  • SD-36
    T186802429877-44-9In house
    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.
    • $970
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  • Stafib-2
    T96462097938-74-2In house
    Stafib-2 is a potent and selective inhibitor of the transcription factor STAT5b.Stafib-2 inhibits STAT5b and STAT5a with IC50 values of 82 nM and 1.7 μM, respectively.Stafib-2 has poor cell permeability.
    • $267
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  • ENMD-1198
    T15234864668-87-1In house
    ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
    • $1,520
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  • STX-0119
    T60160851095-32-4In house
    STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM.
    • $58
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  • C188-9
    T4650432001-19-9
    C188-9 (TTI-101) is a Stat3 inhibitor with an IC50 of 4-7 μM.
    • $38
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  • BP-1-102
    T37081334493-07-0
    BP-1-102 is an orally active, effective and specific STAT3 inhibitor. BP-1-102 binds Stat3 (Kd: 504 nM), then blocks Stat3-phosphotyrosine (pTyr) peptide interactions and Stat3 activation (4-6.8 μM), and selectively inhibits 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.
    • $33
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  • Ochromycinone
    T6995111540-00-2
    Ochromycinone (STA 21) is a selective STAT3 inhibitor.
    • $133
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  • HJC0152 hydrochloride
    T42341420290-99-8
    HJC0152 hydrochloride (HJC0152) is a signal transducer and activator of transcription 3 (STAT3) inhibitor.
    • $33
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  • Scutellarin
    T278927740-01-8
    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.
    • $45
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  • Atractylenolide I
    T5S016773069-13-3
    1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res
    • $36
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  • Diosgenin
    T2867512-04-9
    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.
    • $30
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  • Fludarabine
    T103821679-14-1
    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.
    • $50
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  • Cucurbitacin B
    T34046199-67-3
    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.
    • $44
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  • AG490
    T2600133550-30-8
    AG490 (Tyrphostin B42) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src.
    • $43
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  • 2-(1,8-naphthyridin-2-yl)phenol
    T216865182-56-1
    2-NP is a STAT1 enhancer.
    • $55
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  • WP1066
    T2156857064-38-1
    WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3. WP1066 has been used in trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.
    • $44
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  • Corylifol A
    T4S0145775351-88-7
    1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug/ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.
    • $47
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  • Stattic
    T630819983-44-9
    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.
    • $30
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  • TPCA-1
    T3049507475-17-4
    TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes.
    • $38
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  • Cryptotanshinone
    T281435825-57-1
    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.
    • $46
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  • RO8191
    T22142691868-88-9
    RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.
    • $38
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  • STAT5-IN-1
    T4216285986-31-4
    STAT5-IN-1 (STAT5 Inhibitor) is a cell-permeable inhibitor which suppresses Stat5 via binding to the SH2 domain.
    • $47
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  • Morusin
    T5S160762596-29-6
    1. Morusin (Mulberrochromene) possesses antitumor effects of cell lines including HT-29, A549, MCF-7, and MDA-MB-231, through suppressing STAT3 and NFκB attenuation mediated apoptosis induction. 2. Morusin possesses anti-oxidant and anti-inflammatory effects.
    • $68
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  • Atractylenolide II
    T5S016873069-14-4
    1. Atractylenolide II (2-Atractylenolide) has antimelanoma effect by inhibiting STAT3 signalling. 2. Atractylenolide II has cytotoxic/apoptotic effects may via p38 activation , ERK and Akt inactivation, p53 dependent.
    • $140
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  • AS1517499
    T4476919486-40-1
    AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM
    • $34
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  • Artesunate
    T043388495-63-0
    Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines.
    • $33
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  • NT157
    T46051384426-12-3
    NT157 is a small molecule tyrphostin targeting IRS protein and has the potential to inhibit IGF-1R and STAT3 signaling pathways in TME cancer cells and stromal cells, resulting in decreased cancer cell survival.
    • $50
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  • Icaritin
    T3398118525-40-9
    Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.
    • $30
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  • S3I-201
    T2505501919-59-1
    S3I-201 (S3I-201) is a selective Stat3 inhibitor (IC50: 86±33 μM) and low effect towards STAT1/5.
    • $50
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  • Niclosamide
    T071150-65-7
    Niclosamide (Niclocide)(BAY2353) is used to treat most tapeworm infections by inhibiting DNA replication.
    • $39
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  • BD750
    T8546892686-59-8
    BD750 is an effective immunosuppressant and a JAK3 STAT5 inhibitor, inhibits IL-2-induced JAK3 STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM in mouse and human T cells, respectively)
    • $47
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  • Corylin
    T6S014153947-92-5
    Corylin is a major bioactive compound isolated from Psoralea corylifolia L; it has the activity of antibiotic or anticancer.
    • $70
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  • Homoharringtonine
    T338026833-87-4
    Homoharringtonine (HHT) is a natural alkaloid that inhibits the translation of proteins and is cytotoxic. Homoharringtonine acts on the ribosomes of tumor cells to inhibit the elongation step of protein translation, thereby inhibiting protein synthesis, and has antitumor activity.
    • $50
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  • Colivelin
    TP1856867021-83-8
    Colivelin is a neuroprotective peptide and activator of STAT3. Colivelin is a hybrid peptide synthesized to enhance the neuroprotective effects of humanin (HN).
    • $237
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  • Napabucasin
    T321883280-65-3
    Napabucasin (BBI608) is an orally available Stat3 and Y cell stemness inhibitor.
    • $61
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