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STAT Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S7024 | Stattic | Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis. |
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| S1155 | NSC 74859 (S3I-201) | NSC 74859 (S3I-201) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5. |
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| S1491 | Fludarabine | Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis. |
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| S2285 | Cryptotanshinone (Tanshinone C) | Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibiting phosphorylation of STAT3 Tyr705 with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. It also induces ROS-dependent autophagy and mitochondria-mediated apoptosis. |
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| S8605 | C188-9 (TTI-101) | C188-9 (TTI 101) is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. |
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| S7337 | SH-4-54 | SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively. |
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| S3030 | Niclosamide | Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. This compound selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5). |
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| S7769 | BP-1-102 | BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM. |
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| S7977 | Napabucasin (BBI608) | Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor. |
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| S8685 | AS1517499 | AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. |
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| S4182 | 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. |
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| S7501 | HO-3867 | HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. This compound induces apoptosis. |
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| S9015 | Homoharringtonine (HHT) | Homoharringtonine (HHT), a plant alkaloid with antitumor properties, inhibits protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site. This compound reversiblely inhibits IL-6-induced STAT3 Tyrosine 705 phosphorylation and reduced anti-apoptotic proteins expression. |
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| S6784 | STAT5-IN-1 | STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. |
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| S7951 | Ochromycinone (STA-21) | Ochromycinone (STA-21) is a selective STAT3 inhibitor. |
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| S8561 | HJC0152 | HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility. |
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| S8197 | APTSTAT3-9R | APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of this compound in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets. |
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| S0818 | STAT3-IN-1 | STAT3-IN-1 (compound 7d) is an excellent, selective and orally active inhibitor of STAT3 with IC50 of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. This compound induces apoptosis of tumor cells. |
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| S0986 | SC-1 | SC-1 (1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea, STAT3-IN-7), a Sorafenib analogue and potently inhibits the phosphorylation of STAT3, induces cell apoptosis through SHP-1 dependent STAT3 inactivation. |
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| E1124 | Narciclasine | Narciclasine (Lycoricidinol), an isocarbostyril alkaloid, targets STAT3 via distinct mechanisms in tamoxifen-resistant breast cancer cells. This compound suppresses phosphorylation, activation, dimerization, and nuclear translocation of STAT3 by directly binding with the STAT3 SH2 domain and leads STAT3 degradation. It is a plant growth modulator. This chemical modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner. |
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| S9920 | 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.Stock solutions should be stored under nitrogen, sealed. |
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| E0485 | Stafia-1 | Stafia-1 is the first STAT5a inhibitor that inhibits STAT5a (IC50=22.2 μM, Ki=10.9 μM) with at least 9‐fold selectivity over STAT5b and higher selectivity against other STAT family members. |
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| S7923 | SH5-07 (SH-5-07) | 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. |
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| S3810 | Scutellarin | Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide), the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities. This compound can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. |
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| S0918 | Ginkgolic acid C17:1 | Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. This compound can induce the substantial expression of PTEN and SHP-1. It induces apoptosis of tumor cells. | ||
| E3177 | Centipeda Minima Extract | Centipeda Minima Extract is extracted from the medicinal herb Centipeda minima, has promising anticancer activities. | ||
| S0949 | Cucurbitacin IIb | Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. This compound exhibits anti-inflammatory activity and induces apoptosis. It is isolated from Hemsleya amabilis. | ||
| E5802New | SD-436 | SD-436 is a potent and selective PROTAC degrader of STAT3 with a DC50 of 0.5 μM. It induces complete and long-lasting tumor regression in leukemia and lymphoma xenograft models in mice. | ||
| E1990New | KT-333 | KT-333 is a first-in-class, potent, and selective heterobifunctional degrader of STAT3 that recruits the VHL E3 ligase for ubiquitin-proteasome-mediated degradation. It induces robust antitumor activity in preclinical models of ALK⁺ anaplastic large cell lymphoma (ALCL). | ||
| E2644 | Tetramethylcurcumin | Tetramethylcurcumin (FLLL31), a small-molecule signal transducer and activator of transcription 3 (STAT3) inhibitor derived from curcumin, binds selectively to Janus kinase 2 and the STAT3 Src homology-2 domain, which serve crucial roles in STAT3 dimerization and signal transduction. | ||
| E6482New | STAT3-IN-12 | STAT3-IN-12 is a potent inhibitor of STAT3signaling, by effectively blocking IL-6-induced activation of the JAK/STAT3 pathway. STAT3-IN-12 suppresses cancer cell proliferation and migration, while promoting apoptosis and inducing cell cycle arrest. | ||
| S1349 | SC99 | SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway by docking into the ATP-binding pocket of JAK2, also inhibits phosphorylation of JAK2and STAT3 with no effects on the other kinases associated with STAT3 signaling. | ||
| E6051New | niclosamide ethanolamine | Niclosamide ethanolamine (Niclosamide-olamine, BAY2353 olamine) is a mild mitochondrial uncoupler, anthelmintic agent, and highly potent inhibitor of STAT3 signaling pathway with an IC50 of 0.25 μM. It improves insulin levels, body weight, and muscle wasting, inhibits artery constriction, suppresses PI3K-mTORC1 signaling to block fibroblast proliferation, inhibits TGF-β1-induced EMT and ECM accumulation via the mTORC1-4EBP1 axis, activates noncanonical autophagy to sensitize fibroblasts to apoptosis, and confers renoprotection in diabetic and adriamycin-induced nondiabetic kidney disease models. | ||
| E2398 | STAT5-IN-2 | STAT5-IN-2 inhibits the growth of acute and chronic myeloid leukemia cells and the phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation, with minimal effects on bone marrow stromal cells that play vital functions in the microenvironment of hematopoietic and leukemic cells. | ||
| S0456 | inS3-54-A18 | inS3-54A18 is a potent inhibitor of STAT3 with anti-cancer properties. | ||
| E2794New | Garcinone D | Garcinone D is a natural xanthone from mangosteen, an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 with an IC50 of 28.23 μM. It promotes neural stem cell proliferation via STAT3 and Nrf2/HO-1 activation while inhibiting prostate and breast cancer growth by blocking the CDK2/CyclinE1-mediated cell cycle and can be used in prostate and breast cancer research. | ||
| E6656New | STAT3-IN-13 | STAT3-IN-13 (compound 6f) is a STAT3 inhibitor. It exhibits anti-proliferative activity and binds to the STAT3 SH2 domain with a KD of 0.46 μM. This compound inhibits STAT3 Y705 phosphorylation and downstream target gene expression. In vitro studies show STAT3-IN-13 induces apoptosis, while in vivo experiments demonstrate its ability to suppress tumor growth and metastasis. STAT3-IN-13 has potential applications in cancer research. | ||
| S1014 | SKI-606 (Bosutinib) | Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. |
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| S1396 | Resveratrol (trans-Resveratrol) | Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases（LOX, IC50=2.7 μM）, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
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| S2796 | WP1066 | WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1. |
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| S2824 | TPCA-1 | TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis. |
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| S1229 | Fludarabine (NSC 118218) Phosphate | Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis. |
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| S2265 | Artesunate | Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; this compound is a potent inhibitor of EXP1. |
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| S6898 | RCM-1 | RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. This compound decreases carcinogenesis and nuclear β-catenin. |
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| S4358 | Pimozide | Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. This compound also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. It is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity. |
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| S3292 | (3R,8S)-Falcarindiol | Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. |
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| S0981 | BD750 | BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively. |
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| S6919 | Brevilin A | Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. This compound induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation. |
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| S0915 | Morusin | Morusin (Mulberrochromene) is an inhibitor of NF-κB and STAT3. This compound is a prenylated flavonoid isolated from Marsdenia australis with antitumor, antioxidant, and anti-bacteria properties. | ||
| S3267 | Nicotiflorin (Kaempferol-3-O-rutinoside) | Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity. | ||
| S5554 | Lanatoside C | Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. This compound induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways. | ||
| S8989 | Xanthatin | Xanthatin is a sesquiterpene lactone isolated from Xanthium strumarium leaves, which can inhibit the nuclear factor kappa-B (NF-κB), mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STATs) signaling pathways. | ||
| E0011 | Linderalactone | Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. This compound induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. It can be isolated from Radix linderae. | ||
| E0769 | Ginsenoside Rh4 | Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways. | ||
| E0700 | cucurbitacin E | Cucurbitacin E (α-Elaterin; α-Elaterine), a tetracyclic triterpene derived from the climbing stem of Cucumic melo L, is an inhibitor of JAK2 and STAT3. | ||
| S0445 | SC-43 | SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. This compound reduces p-STAT3 and induces apoptosis with anti-tumor activity. | ||
| S8152 | Cucurbitacin I |
Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3. |
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