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抑制剂选择性比较

特异性亚型抑制剂

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所有产品(36) STAT抑制剂(34) STAT激活剂(1) STAT调节剂(1)

目录号	产品描述	文献引用	实验数据
S1155	S3I-201 S3I-201 (NSC 74859) 有效抑制STAT3的DNA结合活性，IC50为86 μM，而对STAT1和STAT5的抑制活性低。	Cell Rep, 2021, 34(1):108584 PLoS Pathog, 2021, 17(1):e1009091 J Cell Mol Med, 2021, 10.1111/jcmm.16256	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) 是一种新型的双重Src/Abl抑制剂，在无细胞试验中IC50分别为1.2 nM 和 1 nM。Bosutinib也可通过阻滞p-ERK、p-S6和p-STAT3的磷酸化来有效地降低PI3K/AKT/mTOR、MAPK/ERK和JAK/STAT3信号通路的活性。Bosutinib可促进自噬。	Drug Metab Dispos, 2021, 49(1):53-61 Mol Cell, 2020, 80(6):1104-1122.e9 Nat Protoc, 2020, 15(2):421-449	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)在血管平滑肌细胞中是一种STAT1活化抑制剂，特异性降低STAT1蛋白质水平（和mRNA水平），而对其他STATs无此作用。它还是一种DNA合成抑制剂。Fludarabine可诱导凋亡。	Cell Rep, 2021, 34(1):108584 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	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 是一种新型JAK2和STAT3抑制剂，在HEL细胞中IC50分别为2.30 μM和2.43 μM；对JAK2，STAT3，STAT5和ERK1/2具有抑制活性，而对JAK1和JAK3没有作用。WP1066 可诱导凋亡。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具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。	Adv Biol Regul, 2021, S2212-4926(20)30091-9 Nanotheranostics, 2021, 5(1):113-124 Oxid Med Cell Longev, 2020, 2020:4635163	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.
S6919^New	Brevilin A Brevilin A (6-O-Angeloylplenolina) 是一种从Centipeda minima分离得到的倍半萜内酯，是 STAT3 的选择性抑制剂，可通过阻断JAKs酪氨酸激酶结构域 JH1 来减弱 JAKs 的活性。Brevilin A 可通过线粒体途径和 PI3K/AKT/mTOR 失活来诱导结肠腺癌细胞CT26的凋亡和自噬。
S3267^New	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮，可改变受伤神经元的形状和结构，减少凋亡细胞，下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达，并降低Bax免疫反应性，并增加 Bcl-2 蛋白表达和免疫反应性。
S6898^New	RCM-1 RCM-1 是一种 Forkhead box M1 (FOXM1) 的无毒抑制剂，可抑制杯状细胞化生并阻止暴露在过敏原中的小鼠体内的 IL-13 和 STAT6 的信号转导。RCM-1 可减少了癌变和核 β-catenin。
S3292^New	Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) 是一种天然的聚乙炔化合物，存在于伞形科的许多植物中。Falcarindiol 可抑制LPS刺激的 inducible nitric oxide synthase (iNOS)、tumor necrosis factor alpha (TNFα)、interleukin-6 (IL-6) 和 interleukin-1 beta (IL-1β) 的表达。Falcarindiol 可减弱LPS诱导的 JNK、ERK、STAT1 和 STAT3 信号分子的激活。
S0949^New	Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) 可抑制 STAT3、JNK 和 Erk1/2 的磷酸化，而增强 IκB 和 NF-κB 的磷酸化，阻止 NF-κB 的核易位并降低 IκBα 和 TNF-α 的mRNA表达水平。Cucurbitacin IIb 是从Hemsleya amabilis 中分离出来的，具有抗炎活性并可诱导凋亡。
S0918^New	Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) 通过废除上游的 JAK2 和 Src 来抑制 STAT3 的组成性激活。Ginkgolic acid C17:1 可以诱导 PTEN 和 SHP-1 的大量表达。Ginkgolic acid C17:1 诱导肿瘤细胞凋亡。
S0981^New	BD750 BD750 是一种免疫抑制剂，同时也是 JAK3 和 STAT5 的双重抑制剂，可抑制IL-2诱导的JAK3/STAT5依赖性的T细胞增殖，影响小鼠和人T细胞增殖对应的IC50值分别为1.5 μM和1.1 μM。
S0818^New	STAT3-IN-1 STAT3-IN-1 (compound 7d) 是一种出色的、选择性的 STAT3 的口服活性抑制剂，在HT29细胞和MDA-MB 231细胞中的IC50值分别为1.82 μM和2.14 μM。STAT3-IN-1 诱导肿瘤细胞凋亡。
S0445^New	SC-43 SC-43 是索拉非尼sorafenib的衍生物，是一种 Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) 的激动剂，可减少肝纤维化。SC-43 可减少 p-STAT3 并诱导凋亡，具有抗肿瘤的活性。
S6784^New	STAT5-IN-1 STAT5-IN-1 是一种有效的选择性 STAT5 抑制剂，其对于STAT5β亚型的IC50值为47 μM。
S7024	Stattic Stattic 是第一个非肽类STAT3小分子抑制剂，有效抑制STAT3激活和核易位，IC50为5.1 μM，其作用于STAT3的选择性远高于STAT1。Stattic 可诱导凋亡。	Oncogenesis, 2021, 10(1):8 Ecotoxicol Environ Saf, 2021, 208:111693 Cell, 2020, 182(3):685-712.e19	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)是一种IKK-2抑制剂，无细胞试验中IC50为17.9 nM，抑制NF-κB通路，比作用于IKK-1选择性高22倍。TPCA-1 也是 STAT3 的抑制剂并可促进凋亡。	J Cell Mol Med, 2021, 10.1111/jcmm.16316 Nat Med, 2020, 10.1038/s41591-020-1073-3 Cell Death Dis, 2020, 24;11(4):282	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)能够抑制DNA复制，并抑制STAT3，无细胞试验中IC50为0.7 μM。 Niclosamide 选择性地抑制STAT3的磷酸化，对其他同系物如STAT1和STAT5的激活没有明显抑制作用。	Cell Death Dis, 2020, 11(12):1035 Cell Death Dis, 2020, 11(6):466 J Cell Mol Med, 2020, 5	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是可渗透细胞的，口服有效的硝基呋喃类止泻药，有效地抑制细胞内STAT1/3/5转录活性的激活，IC50为3 µM。	Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00019-9 Signal Transduct Target Ther, 2020, Int J Mol Sci, 2020, 21(3)	(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是一种高效的STAT抑制剂，其作用STAT3和STAT5的K_D分别为300 nM和464 nM。	Nat Med, 2020, 10.1038/s41591-020-0926-0 Aging (Albany NY), 2020, 12 Carcinogenesis, 2020, 41(7):993-1004	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 是具有抗病毒和抗肿瘤活性的强心苷。Lanatoside C 通过减弱 MAPK，Wnt，JAK-STAT和PI3K/AKT/mTOR信号通路，诱导G2/M细胞周期停滞并诱导自噬和细胞凋亡。
S8685	AS1517499 AS1517499是一种新型有效的STAT6抑制剂，IC50为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) 是一种口服具有活性的Stat3和癌细胞多能性抑制剂。	Cell Prolif, 2020, 53(1):e12719 Am J Cancer Res, 2020, 1;10(5):1442-1454 J Cell Mol Med, 2020, 10.1111/jcmm.16132
S2265	Artesunate Artesunate (WR-256283) 是一种抗疟类药，作用于小细胞肺癌细胞系H69，IC50为< 5 μM。它是一种潜在的STAT3抑制剂，在体外对癌细胞有选择性细胞毒性作用；是有效的EXP1抑制剂。	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是有效的、具有口服生物活性的、选择性STAT3抑制剂，与STAT3结合亲和力Kd为504 nM.在4-6.8 μM时，抑制Stat3与pTyr肽段的相互作用和STAT3的激活。	Onco Targets Ther, 2021, 14:379-392 Pharmacol Res Perspect, 2021, 9(1):e00704 Oncogene, 2020, 39(20):3997-4013	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 是一种STAT3抑制剂，无细胞试验中IC50为4.6 μM，强烈抑制STAT3 Tyr705磷酸化，对STAT3 Ser727作用效果弱，对STAT1和STAT5没有作用效果。Cryptotanshinone 可诱导ROS依赖的自噬和线粒体介导的凋亡。	J Cell Mol Med, 2021, 10.1111/jcmm.16250 Mol Med Rep, 2021, 23(1)40 Cancer Res, 2020, canres.530.2020	(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是一种强效的异羟肟酸类STAT3抑制剂，在体内外具有抗肿瘤活性。
S9015	Homoharringtonine Homoharringtonine (Omacetaxine mepesuccinate), 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.	Clin Cancer Res, 2020, clincanres.2246.2020 Oncol Rep, 2020, 43(1):113-120 Oncotarget, 2017, 8(24):39064-39076
S7951	Ochromycinone (STA-21) Ochromycinone (STA-21) 是一个选择性的STAT3抑制剂。	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是signal transducer and activator of transcription 3 (STAT3)抑制剂，其溶解度相较于niclosamide有显著的改善。	Cancer Lett, 2019, 10.1016/j.canlet.2019.02.029 Cancer Manag Res, 2018, 10:6857-6867
S3810	Scutellarin Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide)是从中草药黄芩Scutellaria baicalensis和灯盏细辛Erigeron breviscapus中提取的主要活性类黄酮，具有许多药理作用，例如抗氧化、抗肿瘤、抗病毒和抗炎活性。Scutellarin 可以下调HCC细胞中的 STAT3/Girdin/Akt 信号传导，并抑制破骨细胞中RANKL介导的 MAPK 和 NF-κB 信号通路。
S8197	APTSTAT3-9R APTSTAT3-9R是特异的STAT3结合肽段，加上一段可穿透细胞的模体。对多种类型的癌细胞处理以APTSTAT3-9R可阻断STAT3的磷酸化以及减少STAT靶标的表达。	Carcinogenesis, 2020, 41(7):993-1004
S8605	C188-9 C188-9是一种有效的STAT3抑制剂，与STAT3以高亲和力结合，Kd=4.7±0.4 nM。C188-9在小鼠体内耐受良好，具有较好的口服生物利用度，主要富集于肿瘤组织中。	J Clin Invest, 2021, 131(1)135937 Bone Res, 2021, 9(1):6 Int J Cancer, 2020, 10.1002/ijc.32922	(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, 姜黄素的一种类似物, 是选择性的STAT3抑制剂。抑制STAT3的磷酸化、转录和DNA结合活性，而不影响其他活性STATs的表达。HO-3867 可诱导凋亡。	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.
S9664^New	Colivelin Colivelin (CLN) 是一种脑渗透性的神经保护肽，对神经退行性疾病中的 Aβ 沉积，神经元凋亡和突触可塑性缺陷具有有效的长期作用。 Colivelin 是一种 STAT3 的激活剂。
S3745	Balsalazide disodium Balsalazide Disodium 是balsalazide的二钠盐形式，balsalazide是一种口服的对氨水杨酸钠前体药物，在结肠中被酶解、产生抗炎性的美沙拉秦（mesalazine）。Balsalazide Disodium 通过调节 IL-6/STAT3 途径抑制结肠炎相关的癌变。	Front Microbiol, 2020, 10:2936

目录号	产品描述	文献引用	实验数据
S1155	S3I-201 S3I-201 (NSC 74859) 有效抑制STAT3的DNA结合活性，IC50为86 μM，而对STAT1和STAT5的抑制活性低。	Cell Rep,2021, 34(1):108584 PLoS Pathog,2021, 17(1):e1009091 J Cell Mol Med,2021, 10.1111/jcmm.16256	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) 是一种新型的双重Src/Abl抑制剂，在无细胞试验中IC50分别为1.2 nM 和 1 nM。Bosutinib也可通过阻滞p-ERK、p-S6和p-STAT3的磷酸化来有效地降低PI3K/AKT/mTOR、MAPK/ERK和JAK/STAT3信号通路的活性。Bosutinib可促进自噬。	Drug Metab Dispos,2021, 49(1):53-61 Mol Cell,2020, 80(6):1104-1122.e9 Nat Protoc,2020, 15(2):421-449	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)在血管平滑肌细胞中是一种STAT1活化抑制剂，特异性降低STAT1蛋白质水平（和mRNA水平），而对其他STATs无此作用。它还是一种DNA合成抑制剂。Fludarabine可诱导凋亡。	Cell Rep,2021, 34(1):108584 Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19	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 是一种新型JAK2和STAT3抑制剂，在HEL细胞中IC50分别为2.30 μM和2.43 μM；对JAK2，STAT3，STAT5和ERK1/2具有抑制活性，而对JAK1和JAK3没有作用。WP1066 可诱导凋亡。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具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。	Adv Biol Regul,2021, S2212-4926(20)30091-9 Nanotheranostics,2021, 5(1):113-124 Oxid Med Cell Longev,2020, 2020:4635163	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.
S6919^New	Brevilin A Brevilin A (6-O-Angeloylplenolina) 是一种从Centipeda minima分离得到的倍半萜内酯，是 STAT3 的选择性抑制剂，可通过阻断JAKs酪氨酸激酶结构域 JH1 来减弱 JAKs 的活性。Brevilin A 可通过线粒体途径和 PI3K/AKT/mTOR 失活来诱导结肠腺癌细胞CT26的凋亡和自噬。
S3267^New	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮，可改变受伤神经元的形状和结构，减少凋亡细胞，下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达，并降低Bax免疫反应性，并增加 Bcl-2 蛋白表达和免疫反应性。
S6898^New	RCM-1 RCM-1 是一种 Forkhead box M1 (FOXM1) 的无毒抑制剂，可抑制杯状细胞化生并阻止暴露在过敏原中的小鼠体内的 IL-13 和 STAT6 的信号转导。RCM-1 可减少了癌变和核 β-catenin。
S3292^New	Falcarindiol Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) 是一种天然的聚乙炔化合物，存在于伞形科的许多植物中。Falcarindiol 可抑制LPS刺激的 inducible nitric oxide synthase (iNOS)、tumor necrosis factor alpha (TNFα)、interleukin-6 (IL-6) 和 interleukin-1 beta (IL-1β) 的表达。Falcarindiol 可减弱LPS诱导的 JNK、ERK、STAT1 和 STAT3 信号分子的激活。
S0949^New	Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) 可抑制 STAT3、JNK 和 Erk1/2 的磷酸化，而增强 IκB 和 NF-κB 的磷酸化，阻止 NF-κB 的核易位并降低 IκBα 和 TNF-α 的mRNA表达水平。Cucurbitacin IIb 是从Hemsleya amabilis 中分离出来的，具有抗炎活性并可诱导凋亡。
S0918^New	Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) 通过废除上游的 JAK2 和 Src 来抑制 STAT3 的组成性激活。Ginkgolic acid C17:1 可以诱导 PTEN 和 SHP-1 的大量表达。Ginkgolic acid C17:1 诱导肿瘤细胞凋亡。
S0981^New	BD750 BD750 是一种免疫抑制剂，同时也是 JAK3 和 STAT5 的双重抑制剂，可抑制IL-2诱导的JAK3/STAT5依赖性的T细胞增殖，影响小鼠和人T细胞增殖对应的IC50值分别为1.5 μM和1.1 μM。
S0818^New	STAT3-IN-1 STAT3-IN-1 (compound 7d) 是一种出色的、选择性的 STAT3 的口服活性抑制剂，在HT29细胞和MDA-MB 231细胞中的IC50值分别为1.82 μM和2.14 μM。STAT3-IN-1 诱导肿瘤细胞凋亡。
S0445^New	SC-43 SC-43 是索拉非尼sorafenib的衍生物，是一种 Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) 的激动剂，可减少肝纤维化。SC-43 可减少 p-STAT3 并诱导凋亡，具有抗肿瘤的活性。
S6784^New	STAT5-IN-1 STAT5-IN-1 是一种有效的选择性 STAT5 抑制剂，其对于STAT5β亚型的IC50值为47 μM。
S7024	Stattic Stattic 是第一个非肽类STAT3小分子抑制剂，有效抑制STAT3激活和核易位，IC50为5.1 μM，其作用于STAT3的选择性远高于STAT1。Stattic 可诱导凋亡。	Oncogenesis,2021, 10(1):8 Ecotoxicol Environ Saf,2021, 208:111693 Cell,2020, 182(3):685-712.e19	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)是一种IKK-2抑制剂，无细胞试验中IC50为17.9 nM，抑制NF-κB通路，比作用于IKK-1选择性高22倍。TPCA-1 也是 STAT3 的抑制剂并可促进凋亡。	J Cell Mol Med,2021, 10.1111/jcmm.16316 Nat Med,2020, 10.1038/s41591-020-1073-3 Cell Death Dis,2020, 24;11(4):282	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)能够抑制DNA复制，并抑制STAT3，无细胞试验中IC50为0.7 μM。 Niclosamide 选择性地抑制STAT3的磷酸化，对其他同系物如STAT1和STAT5的激活没有明显抑制作用。	Cell Death Dis,2020, 11(12):1035 Cell Death Dis,2020, 11(6):466 J Cell Mol Med,2020, 5	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是可渗透细胞的，口服有效的硝基呋喃类止泻药，有效地抑制细胞内STAT1/3/5转录活性的激活，IC50为3 µM。	Cell Mol Gastroenterol Hepatol,2021, S2352-345X(21)00019-9 Signal Transduct Target Ther,2020, Int J Mol Sci,2020, 21(3)	(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是一种高效的STAT抑制剂，其作用STAT3和STAT5的K_D分别为300 nM和464 nM。	Nat Med,2020, 10.1038/s41591-020-0926-0 Aging (Albany NY),2020, 12 Carcinogenesis,2020, 41(7):993-1004	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 是具有抗病毒和抗肿瘤活性的强心苷。Lanatoside C 通过减弱 MAPK，Wnt，JAK-STAT和PI3K/AKT/mTOR信号通路，诱导G2/M细胞周期停滞并诱导自噬和细胞凋亡。
S8685	AS1517499 AS1517499是一种新型有效的STAT6抑制剂，IC50为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) 是一种口服具有活性的Stat3和癌细胞多能性抑制剂。	Cell Prolif,2020, 53(1):e12719 Am J Cancer Res,2020, 1;10(5):1442-1454 J Cell Mol Med,2020, 10.1111/jcmm.16132
S2265	Artesunate Artesunate (WR-256283) 是一种抗疟类药，作用于小细胞肺癌细胞系H69，IC50为< 5 μM。它是一种潜在的STAT3抑制剂，在体外对癌细胞有选择性细胞毒性作用；是有效的EXP1抑制剂。	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是有效的、具有口服生物活性的、选择性STAT3抑制剂，与STAT3结合亲和力Kd为504 nM.在4-6.8 μM时，抑制Stat3与pTyr肽段的相互作用和STAT3的激活。	Onco Targets Ther,2021, 14:379-392 Pharmacol Res Perspect,2021, 9(1):e00704 Oncogene,2020, 39(20):3997-4013	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 是一种STAT3抑制剂，无细胞试验中IC50为4.6 μM，强烈抑制STAT3 Tyr705磷酸化，对STAT3 Ser727作用效果弱，对STAT1和STAT5没有作用效果。Cryptotanshinone 可诱导ROS依赖的自噬和线粒体介导的凋亡。	J Cell Mol Med,2021, 10.1111/jcmm.16250 Mol Med Rep,2021, 23(1)40 Cancer Res,2020, canres.530.2020	(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是一种强效的异羟肟酸类STAT3抑制剂，在体内外具有抗肿瘤活性。
S9015	Homoharringtonine Homoharringtonine (Omacetaxine mepesuccinate), 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.	Clin Cancer Res,2020, clincanres.2246.2020 Oncol Rep,2020, 43(1):113-120 Oncotarget,2017, 8(24):39064-39076
S7951	Ochromycinone (STA-21) Ochromycinone (STA-21) 是一个选择性的STAT3抑制剂。	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是signal transducer and activator of transcription 3 (STAT3)抑制剂，其溶解度相较于niclosamide有显著的改善。	Cancer Lett,2019, 10.1016/j.canlet.2019.02.029 Cancer Manag Res,2018, 10:6857-6867
S3810	Scutellarin Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide)是从中草药黄芩Scutellaria baicalensis和灯盏细辛Erigeron breviscapus中提取的主要活性类黄酮，具有许多药理作用，例如抗氧化、抗肿瘤、抗病毒和抗炎活性。Scutellarin 可以下调HCC细胞中的 STAT3/Girdin/Akt 信号传导，并抑制破骨细胞中RANKL介导的 MAPK 和 NF-κB 信号通路。
S8197	APTSTAT3-9R APTSTAT3-9R是特异的STAT3结合肽段，加上一段可穿透细胞的模体。对多种类型的癌细胞处理以APTSTAT3-9R可阻断STAT3的磷酸化以及减少STAT靶标的表达。	Carcinogenesis,2020, 41(7):993-1004
S8605	C188-9 C188-9是一种有效的STAT3抑制剂，与STAT3以高亲和力结合，Kd=4.7±0.4 nM。C188-9在小鼠体内耐受良好，具有较好的口服生物利用度，主要富集于肿瘤组织中。	J Clin Invest,2021, 131(1)135937 Bone Res,2021, 9(1):6 Int J Cancer,2020, 10.1002/ijc.32922	(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, 姜黄素的一种类似物, 是选择性的STAT3抑制剂。抑制STAT3的磷酸化、转录和DNA结合活性，而不影响其他活性STATs的表达。HO-3867 可诱导凋亡。	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.

目录号	产品描述	文献引用	实验数据
S9664^New	Colivelin Colivelin (CLN) 是一种脑渗透性的神经保护肽，对神经退行性疾病中的 Aβ 沉积，神经元凋亡和突触可塑性缺陷具有有效的长期作用。 Colivelin 是一种 STAT3 的激活剂。

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S9664^New

Colivelin

Colivelin (CLN) 是一种脑渗透性的神经保护肽，对神经退行性疾病中的 Aβ 沉积，神经元凋亡和突触可塑性缺陷具有有效的长期作用。 Colivelin 是一种 STAT3 的激活剂。

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S3745	Balsalazide disodium Balsalazide Disodium 是balsalazide的二钠盐形式，balsalazide是一种口服的对氨水杨酸钠前体药物，在结肠中被酶解、产生抗炎性的美沙拉秦（mesalazine）。Balsalazide Disodium 通过调节 IL-6/STAT3 途径抑制结肠炎相关的癌变。	Front Microbiol, 2020, 10:2936

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S3745

Balsalazide disodium

Balsalazide Disodium 是balsalazide的二钠盐形式，balsalazide是一种口服的对氨水杨酸钠前体药物，在结肠中被酶解、产生抗炎性的美沙拉秦（mesalazine）。Balsalazide Disodium 通过调节 IL-6/STAT3 途径抑制结肠炎相关的癌变。

Front Microbiol, 2020, 10:2936

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