STAT
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
STAT Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1155 |
S3I-201S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5. |
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).
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| 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. |
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 . |
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| S1491 |
FludarabineFludarabine 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. |
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.
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| S7024 |
StatticStattic, 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. |
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.
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| S3030 |
NiclosamideNiclosamide 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). |
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.
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| S6784New |
STAT5-IN-1STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. |
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| S4182 |
NifuroxazideNifuroxazide 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. |
(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.
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| S7337 |
SH-4-54SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively. |
Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
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| S8685 |
AS1517499AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. |
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| S7977 |
Napabucasin(BBI608)Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor. |
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| S2265 |
ArtesunateArtesunate 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. |
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| S7769 |
BP-1-102BP-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. |
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).
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| S2285 |
CryptotanshinoneCryptotanshinone 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. |
(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.
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| S7923 |
SH5-07 (SH-5-07)SH5-07 is a robust hydroxamic acid-based STAT3 inhibitor, which induce antitumor cell effects in vitro and antitumor response in vivo against human glioma and breast cancer models. |
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| S9015 |
HomoharringtonineHomoharringtonine, 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. |
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| S7951 |
Ochromycinone (STA-21)Ochromycinone (STA-21) is a selective STAT3 inhibitor. |
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| S8561 |
HJC0152HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility. |
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| S3810 |
ScutellarinScutellarin, 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, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. |
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| S8197 |
APTSTAT3-9RAPTSTAT3-9R 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. |
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| S8605 |
C188-9C188-9 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. |
(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;
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| S7501 |
HO-3867HO-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. |
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 |
|---|---|---|---|
| S1155 |
S3I-201S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5. |
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. |
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 |
FludarabineFludarabine 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. |
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 |
StatticStattic, 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. |
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 |
NiclosamideNiclosamide 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). |
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.
|
|
| S6784New |
STAT5-IN-1STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. |
||
| S4182 |
NifuroxazideNifuroxazide 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. |
(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-4-54SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively. |
Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
|
|
| S8685 |
AS1517499AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. |
||
| S7977 |
Napabucasin(BBI608)Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor. |
||
| S2265 |
ArtesunateArtesunate 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. |
||
| S7769 |
BP-1-102BP-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. |
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 |
CryptotanshinoneCryptotanshinone 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. |
(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 |
HomoharringtonineHomoharringtonine, 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. |
||
| S7951 |
Ochromycinone (STA-21)Ochromycinone (STA-21) is a selective STAT3 inhibitor. |
||
| S8561 |
HJC0152HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility. |
||
| S3810 |
ScutellarinScutellarin, 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, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. |
||
| S8197 |
APTSTAT3-9RAPTSTAT3-9R 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. |
||
| S8605 |
C188-9C188-9 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. |
(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;
|
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| S7501 |
HO-3867HO-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. |
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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