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. |
On day 1, 5-week-old female NOD/SCID mice were injected with 1 x 108 cells of the NOD/SCID repopulating T315I BCR-ABL1-positive leukemia UPN1 cells. On day 2, these mice were treated with either vehicle (n = 6), vismodegib (20 mg/kg per os; q.d.; n = 6), ponatinib (30 mg/kg; q.d.; n = 6), vismodegib (20 mg/kg per os; q.d.) + ponatinib (30 mg/kg; q.d.; n = 6) for each group. On day 28, mice were sacrificed for evaluation. CD19-positive cells from peripheral blood from each mouse have been shown. Histopathologic analysis of the bone marrow cavity from each treated mouse with UPN1 transplantation. Similar results were obtained in 2 independent experiments. H&E, hematoxylin and eosin.
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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. |
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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. |
The cell viability was determined in HEC-1B cells treated with MPA, insulin, GSK1904529A or Stattic or with silenced DHCR24. |
|
| 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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| 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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| 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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| 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. |
On day 1, 5-week-old female NOD/SCID mice were injected with 1 x 108 cells of the NOD/SCID repopulating T315I BCR-ABL1-positive leukemia UPN1 cells. On day 2, these mice were treated with either vehicle (n = 6), vismodegib (20 mg/kg per os; q.d.; n = 6), ponatinib (30 mg/kg; q.d.; n = 6), vismodegib (20 mg/kg per os; q.d.) + ponatinib (30 mg/kg; q.d.; n = 6) for each group. On day 28, mice were sacrificed for evaluation. CD19-positive cells from peripheral blood from each mouse have been shown. Histopathologic analysis of the bone marrow cavity from each treated mouse with UPN1 transplantation. Similar results were obtained in 2 independent experiments. H&E, hematoxylin and eosin.
|
|
| 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. |
|
|
| 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. |
The cell viability was determined in HEC-1B cells treated with MPA, insulin, GSK1904529A or Stattic or with silenced DHCR24. |
|
| 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.
|
|
| 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. |
||
| 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. |
||
| 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;
|
|
| 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.
|
