STAT
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| 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 |
| S8685 | AS1517499 | <1 mg/mL | 79 mg/mL | 36 mg/mL |
| S7337 | SH-4-54 | <1 mg/mL | 100 mg/mL | 50 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 |
| S7951 | Ochromycinone (STA-21) | <1 mg/mL | 21 mg/mL | 2 mg/mL |
| S8561 | HJC0152 | <1 mg/mL | 88 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 |
特异性亚型抑制剂
- STAT抑制剂（17）
- 新STAT产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1155 |
S3I-201S3I-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。 |
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。 |
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| S7024 |
StatticStattic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。 |
The cell viability was determined in HEC-1B cells treated with MPA, insulin, GSK1904529A or Stattic or with silenced DHCR24. |
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| S3030 |
NiclosamideNiclosamide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。 |
Bacterial infection in IPEC-J2 cells. The invasion and attachment of EHECO157:H7 was increased in the IPEC-J2 cells in the presence of 1 μM niclosamide. Data are expressed as the mean ± SEM (n= 6). Differences between groups were determined by paired samples t-test. *P<0.05 compared with the control.
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| S4182 |
NifuroxazideNifuroxazide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。 |
(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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| S8685New |
AS1517499AS1517499是一种新型有效的STAT6抑制剂，IC50为21 nM。 |
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| S7337 |
SH-4-54SH-4-54是一种高效的STAT抑制剂，其作用STAT3和STAT5的KD分别为300 nM和464 nM。 |
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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| S7977 |
NapabucasinNapabucasin是一种口服具有活性的Stat3和癌细胞多能性抑制剂。 |
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| S2265 |
ArtesunateArtesunate 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。 |
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| S7769 |
BP-1-102BP-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。 |
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。 |
(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。 |
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| S7951 |
Ochromycinone (STA-21)STA-21是一个选择性的STAT3抑制剂。 |
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| S8561 |
HJC0152HJC0152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。 |
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| S8197 |
APTSTAT3-9RAPTSTAT3-9R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。 |
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| S8605 |
C188-9C188-9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。 |
(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, 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。 |
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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