STAT
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1155 | S3I-201 | <1 mg/mL | 73 mg/mL | <1 mg/mL |
| S1491 | Fludarabine | <1 mg/mL | 57 mg/mL | <1 mg/mL |
| S7024 | Stattic | <1 mg/mL | 42 mg/mL | <1 mg/mL |
| S3030 | Niclosamide | <1 mg/mL | <1 mg/mL | <1 mg/mL |
| S4182 | Nifuroxazide | <1 mg/mL | 55 mg/mL | <1 mg/mL |
| S6784 | STAT5-IN-1 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S7337 | SH-4-54 | <1 mg/mL | 100 mg/mL | 50 mg/mL |
| S8685 | AS1517499 | <1 mg/mL | 79 mg/mL | 36 mg/mL |
| S7977 | Napabucasin | <1 mg/mL | 10 mg/mL | <1 mg/mL |
| S2265 | Artesunate | <1 mg/mL | 77 mg/mL | 77 mg/mL |
| S7769 | BP-1-102 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2285 | Cryptotanshinone | <1 mg/mL | 5 mg/mL | 1 mg/mL |
| S7923 | SH5-07 (SH-5-07) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S9015 | Homoharringtonine | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S7951 | STA-21 | <1 mg/mL | 21 mg/mL | 2 mg/mL |
| S8561 | HJC0152 | <1 mg/mL | 88 mg/mL | <1 mg/mL |
| S3810 | Scutellarin | -1 mg/mL | 50 mg/mL | -1 mg/mL |
| S8197 | APTSTAT3-9R | 98 mg/mL | <1 mg/mL | <1 mg/mL |
| S8605 | C188-9 | <1 mg/mL | 94 mg/mL | 6 mg/mL |
| S7501 | HO-3867 | <1 mg/mL | 13 mg/mL | 6 mg/mL |
亜型選択性的な製品
STAT製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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).
|
|
| 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. |
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. |
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.
|
|
| 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.
|
|
| S6784新 |
STAT5-IN-1STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. |
||
| 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 |
NapabucasinNapabucasin 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, inhibit protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site |
||
| S7951 |
STA-21Ochromycinone (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. |
||
| 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.
|
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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).
|
|
| 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. |
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. |
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.
|
|
| 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.
|
|
| S6784新 |
STAT5-IN-1STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform. |
||
| 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 |
NapabucasinNapabucasin 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, inhibit protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site |
||
| S7951 |
STA-21Ochromycinone (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. |
||
| 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.
|
