STAT

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

STAT Products

All (32) STAT Inhibitors (30) STAT Agonists (1) STAT Modulators (1)

Catalog No.	Information	Product Use Citations	Product Validations
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.	Elife, 2020, 30;9. pii: e51317 Brain Behav Immun, 2020, 84:72-79 Cancers (Basel), 2020, 19;12(3) pii: E726	The inhibitors U0126, PP1 and S3I-201 reduce the colony-forming ability of KIF5B-RET positive cells. A549 cells carrying KIF5B-RET were diluted and seeded in 6-well plates, treated with DMSO, U0126 (MEK inhibitor) 10 uM, PP1 (SRC inhibitors) 5 uM or S3I-201(STAT3 inhibitors) 100 uM for 14 days. The total numbers of colonies, each containing more than 40 cells, were determined. (P < 0.05, P < 0.01, **P < 0.001, Student's t test).
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.	Nat Protoc, 2020, 15(2):421-449 Nat Commun, 2020, 29;11(1):2086 Genome Med, 2020, 18;12(1):17	A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .
S1491	Fludarabine Fludarabine (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.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cell Metab, 2020, 31(3):564-579	Normal human KC pretreated with STAT1 inhibitor (fludarabine [10 uM]) or STAT3 inhibitor (STA-21 [2 uM]) for 24 h. The mRNA levels of hBD2 and hBD3 were assessed by qRT-PCR.
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.	Oncogene, 2020, 9 Carcinogenesis, 2020, 41(7):993-1004 Cell Mol Neurobiol, 2020, 10.1007/s10571-020-00812-7	Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.
S1396	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.	Bone, 2020, 133:115252 J Biol Chem, 2020, 13;295(11):3485-3496 Oncol Lett, 2020, 19(4):3269-3277	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
S3267^New	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.
S6898^New	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.
S3292^New	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.
S0949^New	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.
S0818^New	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.
S6784^New	STAT5-IN-1 STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform.
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.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cell Metab, 2020, 31(2):327-338	Western blot analysis of p-STAT3, total STAT3, ABCA1 and ABCG1 levels in cells pretreated with DMSO or Stattic (10 uM) for 1 hr before and during stimulation with rDKK1 in cells transfected with STAT3 siRNA or negative control, and rDKK1 added into the supernatant.
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.	Cell Death Dis, 2020, 24;11(4):282 Cells, 2020, 9(2) Eur J Pharmacol, 2020, 873:172981	AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
S3030	Niclosamide Niclosamide (Niclocide) 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 Dis, 2020, 11(6):466 J Cell Mol Med, 2020, 5 Biomed J, 2020, S2319-4170(20)30066-4	Effects of some confirmed hits on IRF7 transcription level in response to IFN-α2a treatment (1 h) in SH-SY5Y cells. Data represent mean expression fold±SEM relative to GAPDH, measured from three independent experiments, each in triplicates. P<0.05, P<0.01, and **P<0.001 compared to IFN-α2a treated cells.
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.	Signal Transduct Target Ther, 2020, Int J Mol Sci, 2020, 21(3) Cell Mol Immunol, 2020, 10.1038/s41423-019-0345-7	(A) and (B) NSCs were transfected with vector or shRNA against miR-200a, and then the miR-200a-silenced cells were treated with or without Nifuroxazide. p-STAT1, STAT1, p-STAT3, STAT3 and c-Myc expression levels were determined by Western blotting.
S7337	SH-4-54 SH-4-54 is a potent STAT inhibitor with K_D of 300 nM and 464 nM for STAT3 and STAT5, respectively.	Nat Med, 2020, 10.1038/s41591-020-0926-0 Carcinogenesis, 2020, 41(7):993-1004 Mol Cancer Res, 2020, 10.1158/1541-7786	Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
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.
S8685	AS1517499 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.	Hepatology, 2020, 25 Clin Exp Rheumatol, 2020, 38 Suppl 124(2):69-78 Arch Biochem Biophys, 2020, 685:108330
S7977	Napabucasin(BBI608) Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.	Cell Prolif, 2020, 53(1):e12719 Am J Cancer Res, 2020, 1;10(5):1442-1454 Onco Targets Ther, 2020, 12;13:2215-2224
S2265	Artesunate 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.	J Cell Physiol, 2020, 10.1002 Antiviral Res, 2020, 29:104810 ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00522
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.	Oncogene, 2020, 39(20):3997-4013 Cancer Cell Int, 2020, 20;20:179 Front Pharmacol, 2020, 3;11:386	WT and 4E-BP1/2 DKO cells were treated for 4 h with 10 ng/ml LPS with or without 2 μM BP-1-102 (A) and relative amounts of Nfil3 and sIl1ra mRNAs were quantified using RT-qPCR (normalized to Rpl19).
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.	Cancer Res, 2020, canres.530.2020 Aging (Albany NY), 2020, 12(1):502-517 Oxid Med Cell Longev, 2020,	(a) Effect on STAT3 DNA binding activity of the STAT3 inhibitors cryptotanshinone (CTN) and S31-201 in STAT3 mutant cell lines OCI-Ly12 and OCI-Ly13.2. (b) Effect on cell viability at 48 h of the STAT3 inhibitors cryptotanshinone and S31-201 in OCI-Ly12 and OCI-Ly13.2 cells.
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.
S9015	Homoharringtonine Homoharringtonine, 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.	Oncol Rep, 2020, 43(1):113-120 Oncotarget, 2017, 8(24):39064-39076 Clin Cancer Res, 2016, 22(5):1138-49
S7951	Ochromycinone (STA-21) Ochromycinone (STA-21) is a selective STAT3 inhibitor.	Cell Death Dis, 2020, 19;11(2):135 Cell Death Discov, 2020, 2;6:42 Cancer Genomics Proteomics, 2020, 17(5):517-527
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
S3810	Scutellarin Scutellarin, 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.
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.	Carcinogenesis, 2020, 41(7):993-1004
S8605	C188-9 C188-9 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.	Int J Cancer, 2020, 10.1002/ijc.32922 Cancers (Basel), 2020, 12;12(3) pii: E666 Cell Death Dis, 2020, 14;11(4):230	(E) Hep3B cells were pre-infected with flag-CEP55 for 24 h and were then infected with 10 nM JAK2 inhibitor XL019 or 10 nM STAT3 inhibitor C188-9 for 48 h. Cells’ invasion ability was determined by trans-well assays. Representative microscope images are plotted. Bars, 50 μm;
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.	Oncogene, 2020, 39(20):3997-4013 Carcinogenesis, 2020, 41(7):993-1004 Transl Oncol, 2020, 13(11):100841	Cell apoptosis as measured by TUNEL. Representative sections as determined at 12 hours after reperfusion (3100 magnification). Apoptotic nuclei were stained red, and the software of Image J was used to analyse quantity of TUNEL-positive cells in the livers. Scale bars5100 lm. P<0.05, P<0.01, **P<0.001 compared with IR group.
S0445^New	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.
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

Catalog No.	Information	Product Use Citations	Product Validations
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.	Elife, 2020, 30;9. pii: e51317 Brain Behav Immun, 2020, 84:72-79 Cancers (Basel), 2020, 19;12(3) pii: E726	The inhibitors U0126, PP1 and S3I-201 reduce the colony-forming ability of KIF5B-RET positive cells. A549 cells carrying KIF5B-RET were diluted and seeded in 6-well plates, treated with DMSO, U0126 (MEK inhibitor) 10 uM, PP1 (SRC inhibitors) 5 uM or S3I-201(STAT3 inhibitors) 100 uM for 14 days. The total numbers of colonies, each containing more than 40 cells, were determined. (P < 0.05, P < 0.01, **P < 0.001, Student's t test).
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.	Nat Protoc, 2020, 15(2):421-449 Nat Commun, 2020, 29;11(1):2086 Genome Med, 2020, 18;12(1):17	A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .
S1491	Fludarabine Fludarabine (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.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cell Metab, 2020, 31(3):564-579	Normal human KC pretreated with STAT1 inhibitor (fludarabine [10 uM]) or STAT3 inhibitor (STA-21 [2 uM]) for 24 h. The mRNA levels of hBD2 and hBD3 were assessed by qRT-PCR.
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.	Oncogene, 2020, 9 Carcinogenesis, 2020, 41(7):993-1004 Cell Mol Neurobiol, 2020, 10.1007/s10571-020-00812-7	Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.
S1396	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.	Bone, 2020, 133:115252 J Biol Chem, 2020, 13;295(11):3485-3496 Oncol Lett, 2020, 19(4):3269-3277	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
S3267^New	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.
S6898^New	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.
S3292^New	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.
S0949^New	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.
S0818^New	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.
S6784^New	STAT5-IN-1 STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform.
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.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Cell Metab, 2020, 31(2):327-338	Western blot analysis of p-STAT3, total STAT3, ABCA1 and ABCG1 levels in cells pretreated with DMSO or Stattic (10 uM) for 1 hr before and during stimulation with rDKK1 in cells transfected with STAT3 siRNA or negative control, and rDKK1 added into the supernatant.
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.	Cell Death Dis, 2020, 24;11(4):282 Cells, 2020, 9(2) Eur J Pharmacol, 2020, 873:172981	AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
S3030	Niclosamide Niclosamide (Niclocide) 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 Dis, 2020, 11(6):466 J Cell Mol Med, 2020, 5 Biomed J, 2020, S2319-4170(20)30066-4	Effects of some confirmed hits on IRF7 transcription level in response to IFN-α2a treatment (1 h) in SH-SY5Y cells. Data represent mean expression fold±SEM relative to GAPDH, measured from three independent experiments, each in triplicates. P<0.05, P<0.01, and **P<0.001 compared to IFN-α2a treated cells.
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.	Signal Transduct Target Ther, 2020, Int J Mol Sci, 2020, 21(3) Cell Mol Immunol, 2020, 10.1038/s41423-019-0345-7	(A) and (B) NSCs were transfected with vector or shRNA against miR-200a, and then the miR-200a-silenced cells were treated with or without Nifuroxazide. p-STAT1, STAT1, p-STAT3, STAT3 and c-Myc expression levels were determined by Western blotting.
S7337	SH-4-54 SH-4-54 is a potent STAT inhibitor with K_D of 300 nM and 464 nM for STAT3 and STAT5, respectively.	Nat Med, 2020, 10.1038/s41591-020-0926-0 Carcinogenesis, 2020, 41(7):993-1004 Mol Cancer Res, 2020, 10.1158/1541-7786	Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
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.
S8685	AS1517499 AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.	Hepatology, 2020, 25 Clin Exp Rheumatol, 2020, 38 Suppl 124(2):69-78 Arch Biochem Biophys, 2020, 685:108330
S7977	Napabucasin(BBI608) Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.	Cell Prolif, 2020, 53(1):e12719 Am J Cancer Res, 2020, 1;10(5):1442-1454 Onco Targets Ther, 2020, 12;13:2215-2224
S2265	Artesunate 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.	J Cell Physiol, 2020, 10.1002 Antiviral Res, 2020, 29:104810 ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00522
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.	Oncogene, 2020, 39(20):3997-4013 Cancer Cell Int, 2020, 20;20:179 Front Pharmacol, 2020, 3;11:386	WT and 4E-BP1/2 DKO cells were treated for 4 h with 10 ng/ml LPS with or without 2 μM BP-1-102 (A) and relative amounts of Nfil3 and sIl1ra mRNAs were quantified using RT-qPCR (normalized to Rpl19).
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.	Cancer Res, 2020, canres.530.2020 Aging (Albany NY), 2020, 12(1):502-517 Oxid Med Cell Longev, 2020,	(a) Effect on STAT3 DNA binding activity of the STAT3 inhibitors cryptotanshinone (CTN) and S31-201 in STAT3 mutant cell lines OCI-Ly12 and OCI-Ly13.2. (b) Effect on cell viability at 48 h of the STAT3 inhibitors cryptotanshinone and S31-201 in OCI-Ly12 and OCI-Ly13.2 cells.
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.
S9015	Homoharringtonine Homoharringtonine, 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.	Oncol Rep, 2020, 43(1):113-120 Oncotarget, 2017, 8(24):39064-39076 Clin Cancer Res, 2016, 22(5):1138-49
S7951	Ochromycinone (STA-21) Ochromycinone (STA-21) is a selective STAT3 inhibitor.	Cell Death Dis, 2020, 19;11(2):135 Cell Death Discov, 2020, 2;6:42 Cancer Genomics Proteomics, 2020, 17(5):517-527
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
S3810	Scutellarin Scutellarin, 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.
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.	Carcinogenesis, 2020, 41(7):993-1004
S8605	C188-9 C188-9 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.	Int J Cancer, 2020, 10.1002/ijc.32922 Cancers (Basel), 2020, 12;12(3) pii: E666 Cell Death Dis, 2020, 14;11(4):230	(E) Hep3B cells were pre-infected with flag-CEP55 for 24 h and were then infected with 10 nM JAK2 inhibitor XL019 or 10 nM STAT3 inhibitor C188-9 for 48 h. Cells’ invasion ability was determined by trans-well assays. Representative microscope images are plotted. Bars, 50 μm;
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.	Oncogene, 2020, 39(20):3997-4013 Carcinogenesis, 2020, 41(7):993-1004 Transl Oncol, 2020, 13(11):100841	Cell apoptosis as measured by TUNEL. Representative sections as determined at 12 hours after reperfusion (3100 magnification). Apoptotic nuclei were stained red, and the software of Image J was used to analyse quantity of TUNEL-positive cells in the livers. Scale bars5100 lm. P<0.05, P<0.01, **P<0.001 compared with IR group.

Catalog No.	Information	Product Use Citations	Product Validations
S0445^New	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.

Catalog No.

Information

Product Use Citations

Product Validations

S0445^New

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.

Catalog No.	Information	Product Use Citations	Product Validations
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

Catalog No.

Information

Product Use Citations

Product Validations

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