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STAT Signaling Pathway Map

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  • New STAT Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0011New 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. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
E0485New 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.
E1124New Narciclasine Narciclasine (Lycoricidinol), an isocarbostyril alkaloid narciclasine, targets STAT3 via distinct mechanisms in tamoxifen-resistant breast cancer cells. Narciclasine suppresses phosphorylation, activation, dimerization, and nuclear translocation of STAT3 by directly binding with the STAT3 SH2 domain and leads STAT3 degradation. Narciclasine is a plant growth modulator. Narciclasine 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.
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. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.
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. STAT3-IN-1 induces apoptosis of tumor cells.
Theranostics, 2022, 12(2):842-858
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. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
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. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
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.
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) 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.
J Immunother Cancer, 2022, 10(1)e003766
Front Oncol, 2022, 12:802482
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S1155 S3I-201 S3I-201 (NSC 74859) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.
Cell Death Differ, 2022, 10.1038/s41418-021-00926-5
Cancer Commun (Lond), 2022, 42(3):205-222
Oncoimmunology, 2022, 11(1):2021619
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-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.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1491 Fludarabine (NSC 118218) Fludarabine (NSC 118218, FaraA, Fludarabinum) 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.
Signal Transduct Target Ther, 2022, 7(1):80
Cancers (Basel), 2022, 14(6)1489
iScience, 2022, 25(2):103785
S2265 Artesunate (WR-256283) Artesunate (WR-256283) 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; A potent inhibitor of EXP1.
Front Pharmacol, 2021, 12:615889
Sci Rep, 2021, 11(1):14571
Oncol Lett, 2021, 22(2):597
S2285 Cryptotanshinone Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Adv Sci (Weinh), 2022, e2200263
Front Immunol, 2021, 12:712781
Int J Biol Sci, 2021, 17(10):2417-2429
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.
Cell Biosci, 2022, 12(1):43
Commun Biol, 2022, 5(1):105
Cell Death Differ, 2021, 10.1038/s41418-021-00880-2
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.
Nat Cell Biol, 2022, 24(5):766-782
Sci Adv, 2022, 8(12):eabh4050
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S3030 Niclosamide (BAY2353) Niclosamide (BAY2353, Niclocide, NSC 178296) can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
Cell Death Differ, 2021, 10.1038/s41418-021-00781-4
Cell Death Dis, 2021, 12(9):799
Biochim Biophys Acta Mol Cell Res, 2021, 1868(10):119080
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-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.
S3292 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.
Front Pharmacol, 2021, 12:656697
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. Scutellarin can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
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.
J Immunother Cancer, 2021, 9(6)e002305
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9
Signal Transduct Target Ther, 2020,
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. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S6784 STAT5-IN-1 STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform.
Biomed Pharmacother, 2021, 143:112204
Am J Transl Res, 2021, 13(3):1422-1431
Am J Transl Res, 2021, 13(3):1422-1431
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. RCM-1 decreases carcinogenesis and nuclear β-catenin.
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. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
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.
Nat Commun, 2022, 13(1):791
Haematologica, 2022, 10.3324/haematol.2021.279957
Br J Cancer, 2022, 10.1038/s41416-022-01794-7
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.
Cell Death Dis, 2022, 13(5):424
Diabetes Res Clin Pract, 2022, S0168-8227(22)00588-5
Endocrinology, 2022, 163(5)bqac031
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. HO-3867 induces apoptosis.
Sci Rep, 2022, 12(1):7
Nature, 2021, 600(7888):314-318
Acta Pharm Sin B, 2021, 11(2):394-405
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.
Cell Death Dis, 2022, 13(5):424
Front Immunol, 2021, 12:779667
J Drug Target, 2021, 1-25
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.
S7951 Ochromycinone (STA-21) Ochromycinone (STA-21) is a selective STAT3 inhibitor.
Biochem Pharmacol, 2021, 192:114688
Cell Death Dis, 2020, 19;11(2):135
Cell Death Discov, 2020, 2;6:42
S7977 Napabucasin (BBI608) Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.
Cell Rep Med, 2022, 3(2):100526
Oncogene, 2021, 10.1038/s41388-021-01817-2
Br J Cancer, 2021, 10.1038/s41416-021-01270-8
S8152New 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.

S8197 APTSTAT3-9R APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of APTSTAT3-9R in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets.
Sci Rep, 2022, 12(1):7
Toxicol Mech Methods, 2021, 1-11
Clin Transl Med, 2021, 11(2):e295
S8561 HJC0152 HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
Cancer Lett, 2019, 10.1016/j.canlet.2019.02.029
Cancer Manag Res, 2018, 10:6857-6867
S8605 C188-9 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cancer Immunol Res, 2022, 10(1):56-69
Int J Mol Sci, 2022, 23(4)2019
S8685 AS1517499 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.
BMC Med, 2022, 20(1):148
Cell Death Dis, 2022, 13(1):66
Theranostics, 2021, 11(9):4251-4261
S9015 Homoharringtonine (CGX-635) Homoharringtonine (CGX-635, Omacetaxine mepesuccinate, HHT, Myelostat, NSC 141633), 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. Homoharringtonine reversiblely inhibits IL-6-induced STAT3 Tyrosine 705 phosphorylation and reduced anti-apoptotic proteins expression.
Autophagy, 2022, 1-19
Elife, 2022, 11e71880
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S9920New 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.
A5003 STAT5b Rabbit Recombinant mAb

STAT5b Rabbit Recombinant mAb detects endogenous levels of STAT5b.

A5042 STAT5a Rabbit Recombinant mAb

STAT5a Antibody detects endogenous levels of total STAT5a.

A5044 STAT2 Rabbit Recombinant mAb

STAT2 Antibody detects endogenous levels of STAT2.

A5045 STAT4 Rabbit Recombinant mAb

STAT4 Antibody detects endogenous levels of STAT4.

S9664 Colivelin Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3.
J Reprod Immunol, 2022, 151:103623
Exp Eye Res, 2021, 213:108823
S3745 Balsalazide disodium Balsalazide Disodium is the disodium salt form of balsalazide, an aminosalicylate and oral prodrug that is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide Disodium suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Front Microbiol, 2020, 10:2936
S4842 Balsalazide Balsalazide (Colazal, Giazo), an aminosalicylate and oral prodrug, is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
E0011New 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. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
E0485New 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.
E1124New Narciclasine Narciclasine (Lycoricidinol), an isocarbostyril alkaloid narciclasine, targets STAT3 via distinct mechanisms in tamoxifen-resistant breast cancer cells. Narciclasine suppresses phosphorylation, activation, dimerization, and nuclear translocation of STAT3 by directly binding with the STAT3 SH2 domain and leads STAT3 degradation. Narciclasine is a plant growth modulator. Narciclasine 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.
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. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.
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. STAT3-IN-1 induces apoptosis of tumor cells.
Theranostics, 2022, 12(2):842-858
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. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
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. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
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.
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) 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.
J Immunother Cancer, 2022, 10(1)e003766
Front Oncol, 2022, 12:802482
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S1155 S3I-201 S3I-201 (NSC 74859) shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.
Cell Death Differ, 2022, 10.1038/s41418-021-00926-5
Cancer Commun (Lond), 2022, 42(3):205-222
Oncoimmunology, 2022, 11(1):2021619
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-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.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1491 Fludarabine (NSC 118218) Fludarabine (NSC 118218, FaraA, Fludarabinum) 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.
Signal Transduct Target Ther, 2022, 7(1):80
Cancers (Basel), 2022, 14(6)1489
iScience, 2022, 25(2):103785
S2265 Artesunate (WR-256283) Artesunate (WR-256283) 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; A potent inhibitor of EXP1.
Front Pharmacol, 2021, 12:615889
Sci Rep, 2021, 11(1):14571
Oncol Lett, 2021, 22(2):597
S2285 Cryptotanshinone Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Adv Sci (Weinh), 2022, e2200263
Front Immunol, 2021, 12:712781
Int J Biol Sci, 2021, 17(10):2417-2429
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.
Cell Biosci, 2022, 12(1):43
Commun Biol, 2022, 5(1):105
Cell Death Differ, 2021, 10.1038/s41418-021-00880-2
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.
Nat Cell Biol, 2022, 24(5):766-782
Sci Adv, 2022, 8(12):eabh4050
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S3030 Niclosamide (BAY2353) Niclosamide (BAY2353, Niclocide, NSC 178296) can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
Cell Death Differ, 2021, 10.1038/s41418-021-00781-4
Cell Death Dis, 2021, 12(9):799
Biochim Biophys Acta Mol Cell Res, 2021, 1868(10):119080
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-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.
S3292 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.
Front Pharmacol, 2021, 12:656697
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. Scutellarin can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
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.
J Immunother Cancer, 2021, 9(6)e002305
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9
Signal Transduct Target Ther, 2020,
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. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S6784 STAT5-IN-1 STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform.
Biomed Pharmacother, 2021, 143:112204
Am J Transl Res, 2021, 13(3):1422-1431
Am J Transl Res, 2021, 13(3):1422-1431
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. RCM-1 decreases carcinogenesis and nuclear β-catenin.
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. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
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.
Nat Commun, 2022, 13(1):791
Haematologica, 2022, 10.3324/haematol.2021.279957
Br J Cancer, 2022, 10.1038/s41416-022-01794-7
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.
Cell Death Dis, 2022, 13(5):424
Diabetes Res Clin Pract, 2022, S0168-8227(22)00588-5
Endocrinology, 2022, 163(5)bqac031
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. HO-3867 induces apoptosis.
Sci Rep, 2022, 12(1):7
Nature, 2021, 600(7888):314-318
Acta Pharm Sin B, 2021, 11(2):394-405
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.
Cell Death Dis, 2022, 13(5):424
Front Immunol, 2021, 12:779667
J Drug Target, 2021, 1-25
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.
S7951 Ochromycinone (STA-21) Ochromycinone (STA-21) is a selective STAT3 inhibitor.
Biochem Pharmacol, 2021, 192:114688
Cell Death Dis, 2020, 19;11(2):135
Cell Death Discov, 2020, 2;6:42
S7977 Napabucasin (BBI608) Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.
Cell Rep Med, 2022, 3(2):100526
Oncogene, 2021, 10.1038/s41388-021-01817-2
Br J Cancer, 2021, 10.1038/s41416-021-01270-8
S8152New 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.

S8197 APTSTAT3-9R APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of APTSTAT3-9R in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets.
Sci Rep, 2022, 12(1):7
Toxicol Mech Methods, 2021, 1-11
Clin Transl Med, 2021, 11(2):e295
S8561 HJC0152 HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
Cancer Lett, 2019, 10.1016/j.canlet.2019.02.029
Cancer Manag Res, 2018, 10:6857-6867
S8605 C188-9 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cancer Immunol Res, 2022, 10(1):56-69
Int J Mol Sci, 2022, 23(4)2019
S8685 AS1517499 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.
BMC Med, 2022, 20(1):148
Cell Death Dis, 2022, 13(1):66
Theranostics, 2021, 11(9):4251-4261
S9015 Homoharringtonine (CGX-635) Homoharringtonine (CGX-635, Omacetaxine mepesuccinate, HHT, Myelostat, NSC 141633), 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. Homoharringtonine reversiblely inhibits IL-6-induced STAT3 Tyrosine 705 phosphorylation and reduced anti-apoptotic proteins expression.
Autophagy, 2022, 1-19
Elife, 2022, 11e71880
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S9920New 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.
A5003 STAT5b Rabbit Recombinant mAb

STAT5b Rabbit Recombinant mAb detects endogenous levels of STAT5b.

A5042 STAT5a Rabbit Recombinant mAb

STAT5a Antibody detects endogenous levels of total STAT5a.

A5044 STAT2 Rabbit Recombinant mAb

STAT2 Antibody detects endogenous levels of STAT2.

A5045 STAT4 Rabbit Recombinant mAb

STAT4 Antibody detects endogenous levels of STAT4.

S9664 Colivelin Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3.
J Reprod Immunol, 2022, 151:103623
Exp Eye Res, 2021, 213:108823
S3745 Balsalazide disodium Balsalazide Disodium is the disodium salt form of balsalazide, an aminosalicylate and oral prodrug that is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide Disodium suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Front Microbiol, 2020, 10:2936
S4842 Balsalazide Balsalazide (Colazal, Giazo), an aminosalicylate and oral prodrug, is enzymatically cleaved in the colon to produce the anti-inflammatory agent mesalazine. Balsalazide suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
E0011New 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. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
E0485New 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.
E1124New Narciclasine Narciclasine (Lycoricidinol), an isocarbostyril alkaloid narciclasine, targets STAT3 via distinct mechanisms in tamoxifen-resistant breast cancer cells. Narciclasine suppresses phosphorylation, activation, dimerization, and nuclear translocation of STAT3 by directly binding with the STAT3 SH2 domain and leads STAT3 degradation. Narciclasine is a plant growth modulator. Narciclasine 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.
S8152New 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.

S9920New 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.
Tags: STAT inhibition | STAT signaling pathway | STAT pathway | STAT cancer | STAT signaling | STAT protein | STAT activation | JAK-STAT signaling pathway | STAT3 pathway | STAT3 cancer | STAT3 inhibition | STAT3 activation | STAT phosphorylation | STAT3 protein | STAT1 inhibition | STAT1 pathway | STAT1 activation | STAT1 protein | JAK-STAT mechanism | STAT3 inhibitors in clinical trials | STAT3 inhibitor in vivo | STAT inhibitor review