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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.

Balsalazide disodium dihydrate
T4615150399-21-6
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].
  • $39
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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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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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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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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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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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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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AS2863619
T83782241300-51-4
AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8 19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector memory T cells into Foxp3+ regulatory T cells to study various immune diseases.
  • $133
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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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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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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.
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Solamargine
T403420311-51-7
Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.
  • $54
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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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Angoline
TN673921080-31-9
Angoline (6-Methoxyldihydrochelerythrine) hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor(IC50 : 11.56 μM). It inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
  • $60
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SC-43
T84781400989-25-4
SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.
  • $96
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NT219
T621051198078-60-2In house
NT219 is a dual inhibitor of insulin receptor substrate 1/2 (IRS1/2) and STAT3, enhances the aggregation of misfolded prion protein NT219 affects the levels of certain molecular chaperones and inhibits STAT3 phosphorylation NT219 is useful for the study of cancer and neurodegenerative diseases.
  • $132
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HODHBt
T2126728230-32-2
HODHBt is a STAT5-SUMO protein-protein interaction inhibitor.
  • $39
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AS1517499
T4476919486-40-1
AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM
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Eriocalyxin B
TN162084745-95-9
Eriocalyxin B induces apoptosis and cell cycle arrest in pancreatic adenocarcinoma cells through caspase- and p53-dependent pathways, should be considered a candidate for pancreatic cancer treatment; it is a specific inhibitor of STAT3, it directly target
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AS1810722
T9043909561-15-5
AS1810722, a fused bicyclic pyrimidine derivative, is an orally active and potent inhibitor of STAT6, demonstrating an IC50 of 1.9 nM. It exhibits effective inhibition of CYP3A4, positioning it as a promising candidate for research into allergic diseases, including asthma and atopic conditions.
  • $106
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Saikosaponin D
T391320874-52-6
Saikosaponin D is a novel SERCA inhibitor by inhibiting NF-κB and STAT3 signaling to protect against acetaminophen-induced hepatotoxicity.
  • $47
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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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Casticin
T6S1373479-91-4
1. Casticin (Vitexicarpin) can significantly reduce vascular inflammation, through inhibition of ROS-NF-κB pathway in vascular endothelial cells. 2. Casticin may become a potential leading drug in the therapy of prostate carcinoma.
  • $31
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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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SH-4-54
T66691456632-40-8
SH-4-54 is a most potent, small molecule, nonphosphorylated STAT3 inhibitor.
  • $43
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Ponicidin
T2S197552617-37-5
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens that exhibits immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer activity. Ponicidin induces apoptosis of gastric carcinoma cells, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on the protein levels of JAK2 and STAT3.
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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.
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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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SD-36 TFA
T18680L In house
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.
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Jolkinolide B
T2S104037905-08-1
Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.
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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.
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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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Pimozide
T25462062-78-4
Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.
  • $31
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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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Kurarinone
T5S099334981-26-5
Kurarinone is a flavonoid extracted from the shrub Sophora flavescens, which has anti-tumor, estrogenic and anti-inflammatory activities, and also has a strong inhibitory effect on immune responses.
  • $39
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Sophocarpine
T66776483-15-4
Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
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ML115
T35544912798-42-6
ML115 is a potent and selective activator of transcription 3 (STAT3), with abn EC50 of 2.0 nM, and is inactive against the related STAT1 and NFκB anti-targets.
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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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Cucurbitacin I
TQ01962222-07-3
Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2 STAT3 with anti-cancer activity.
  • $77
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BP-1-102
T37081334493-07-0
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].
  • $33
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Niclosamide
T071150-65-7
Niclosamide (Niclocide)(BAY2353) is used to treat most tapeworm infections by inhibiting DNA replication.
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Stafia-1
T93392582757-90-0
Stafia-1 is a potent STAT5a inhibitor (IC50=22.2 μM), displaying high selectivity over STAT5b and other STAT family members.
  • $78
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STAT3-IN-13
T624912248552-86-3
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.
  • $196
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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.
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Ochromycinone
T6995111540-00-2
Ochromycinone (STA 21) is a selective STAT3 inhibitor.
  • $98
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Alantolactone
T2896546-43-0
Alantolactone is a selective inhibitor of STAT3 that induces cancer-associated apoptosis and has antitumor activity.
  • $50
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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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IST5-002
T6249613484-66-7
IST5-002 (N6-Benzyladenosine-5'-phosphate) is a selective Stat5a b inhibitor with anticancer activity that inhibits the transcriptional activity of Stat5a b and induces apoptosis and death of prostate cancer cells and chronic myelogenous leukemia (CML) cells, which can be used for cancer research.
  • $1,520
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