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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 STAT抑制剂(17)

产品目录	产品描述	文献引用	实验数据
S1155	S3I-201 S3I-201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。	Redox Biol, 2019, 24:101189 Cancers (Basel), 2019, 11(1) Cell Death Dis, 2019, 10(2):104	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).
S1491	Fludarabine Fludarabine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。	Nat Chem Biol, 2019, 15(3):232-240 Nat Commun, 2019, 10(1):2189 Mucosal Immunol, 2019, 10.1038/s41385-019-0178-9	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.
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。	Mol Cancer, 2019, 18(1):40 Diabetes, 2019, 68(6):1303-1314 Redox Biol, 2019, 24:101189	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.
S3030	Niclosamide Niclosamide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。	Oncol Rep, 2019, 41(4):2389-2395 Eur Rev Med Pharmacol Sci, 2019, 23(3):1055-1062 Acta Pharm Sin B, 2018, 8(6):889-899	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。	Cancer Cell Int, 2019, 19:175 PLoS One, 2017, 12(2):e0172178 Onco Targets Ther, 2017, 10:1767-1776	(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。	Cell, 2019, 178(1):160-175 Cell, 2019, 178(1):160-175 Immunobiology, 2019, 224(3):388-396	Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
S8685	AS1517499 AS1517499是一种新型有效的STAT6抑制剂，IC50为21 nM。	Biochem Biophys Res Commun, 2018, 506(1):278-283
S7977	Napabucasin(BBI608) Napabucasin是一种口服具有活性的Stat3和癌细胞多能性抑制剂。	Nat Commun, 2019, 10(1):2131 Int J Gynecol Cancer, 2017, 27(8):1701-1707
S2265	Artesunate Artesunate 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。
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。	Cell, 2019, 178(1):160-175 Cell, 2019, 178(1):160-175 Kidney Blood Press Res, 2019, 44(2):179-187	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。	Redox Biol, 2019, 24:101189 Cancer Manag Res, 2019, 11:5147-5156 Biotechnol Lett, 2019, 41(6-7):733-742	(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。
S7951	Ochromycinone (STA-21) STA-21是一个选择性的STAT3抑制剂。	Thyroid, 2019, 29(5):674-682 Am J Respir Cell Mol Biol, 2019, 10.1165/rcmb.2018-0328OC
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
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。
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。	Front Oncol, 2019, 9:436 Cells, 2018, 7(8)	(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。	Cancer Immunol Res, 2019, 7(5):813-827 Aging (Albany NY), 2019, 11(2):771-782 Cancer Lett, 2018, 433:147-155	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.

产品目录	产品描述	文献引用	实验数据
S1155	S3I-201 S3I-201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。	Redox Biol,2019, 24:101189 Cancers (Basel),2019, 11(1) Cell Death Dis,2019, 10(2):104	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).
S1491	Fludarabine Fludarabine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。	Nat Chem Biol,2019, 15(3):232-240 Nat Commun,2019, 10(1):2189 Mucosal Immunol,2019, 10.1038/s41385-019-0178-9	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.
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。	Mol Cancer,2019, 18(1):40 Diabetes,2019, 68(6):1303-1314 Redox Biol,2019, 24:101189	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.
S3030	Niclosamide Niclosamide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。	Oncol Rep,2019, 41(4):2389-2395 Eur Rev Med Pharmacol Sci,2019, 23(3):1055-1062 Acta Pharm Sin B,2018, 8(6):889-899	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。	Cancer Cell Int,2019, 19:175 PLoS One,2017, 12(2):e0172178 Onco Targets Ther,2017, 10:1767-1776	(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。	Cell,2019, 178(1):160-175 Cell,2019, 178(1):160-175 Immunobiology,2019, 224(3):388-396	Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
S8685	AS1517499 AS1517499是一种新型有效的STAT6抑制剂，IC50为21 nM。	Biochem Biophys Res Commun,2018, 506(1):278-283
S7977	Napabucasin(BBI608) Napabucasin是一种口服具有活性的Stat3和癌细胞多能性抑制剂。	Nat Commun,2019, 10(1):2131 Int J Gynecol Cancer,2017, 27(8):1701-1707
S2265	Artesunate Artesunate 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。
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。	Cell,2019, 178(1):160-175 Cell,2019, 178(1):160-175 Kidney Blood Press Res,2019, 44(2):179-187	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。	Redox Biol,2019, 24:101189 Cancer Manag Res,2019, 11:5147-5156 Biotechnol Lett,2019, 41(6-7):733-742	(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。
S7951	Ochromycinone (STA-21) STA-21是一个选择性的STAT3抑制剂。	Thyroid,2019, 29(5):674-682 Am J Respir Cell Mol Biol,2019, 10.1165/rcmb.2018-0328OC
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
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。
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。	Front Oncol,2019, 9:436 Cells,2018, 7(8)	(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。	Cancer Immunol Res,2019, 7(5):813-827 Aging (Albany NY),2019, 11(2):771-782 Cancer Lett,2018, 433:147-155	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.

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