GANT 58
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GANT58是GLI的拮抗剂，抑制GLI1诱导转录，IC50值为5 μM。
GLI1是属于GLI蛋白家族的人类胶质母细胞瘤分离蛋白。GLI蛋白充当Hedgehog信号通路的效应物，参与胚胎发育过程中细胞的增殖、确定和分型。
GANT58抑制GLI1介导的基因反式激活，对于Hedgehog信号通路具有高选择性。GANT58可以抑制TNF signaling / NFkB的活化、糖皮质激素受体基因的转录和RAS-RAF-MEK-MAPK级联反应。用10 μM的GANT58处理经SAG预处理的SHH-L2细胞48小时后，Hedgehog信号通路减少，而10 μM GANT58 处理2-3天后，GLI1 mRNA水平下降。GANT58被确认为Hedgehog信号通路下游Sufu和Smo的抑制剂[1]。此外，在CCRFeCEM、CEM7e14、CEM1e15和Jurkat细胞中，GANT58处理48小时以剂量依赖的方式引起了细胞生存力的下降。当用10 μM的GANT58处理CCRFeCEM细胞48小时后，停留在G1/S期的细胞比例增加，而在G2/M期细胞比例下降[2]。
在异源移植的小鼠模型中，每天注射GANT 58明显抑制肿瘤生长，注射GANT 58药物18天后，移植物的生长以及肿瘤体积的增长被抑制，实验过程中没有副作用。
参考文献：
[1] Lauth M, Bergstr?m ?sa, Shimokawa T, Toftg?rd R. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proceedings of the National Academy of Sciences of the United States of America. 2007,104(20):8455-8460.
[2] Hou X, Chen X, Zhang P, et al. Inhibition of hedgehog signaling by GANT58 induces apoptosis and shows synergistic antitumor activity with AKT inhibitor in acute T cell leukemia cells. Biochimie. 2014, 101:50-9
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 392.48 |
| Cas No. | 64048-12-0 |
| Formula | C24H16N4S |
| Synonyms | NSC 75503;GANT58;GANT-58;NSC-75503 |
| Solubility | insoluble in H2O; ≥14.9 mg/mL in EtOH with gentle warming and ultrasonic; ≥18.95 mg/mL in DMSO |
| Chemical Name | 4-(2,4,5-tripyridin-4-ylthiophen-3-yl)pyridine |
| SDF | Download SDF |
| Canonical SMILES | C1=CN=CC=C1C2=C(SC(=C2C3=CC=NC=C3)C4=CC=NC=C4)C5=CC=NC=C5 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
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Cell lines |
Shh-L2 cells |
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Reaction Conditions |
10 μM GANT 58 |
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Applications |
When SAG-treated Shh-L2 cells were treated with 10 μM GANT 58 for 48 hours, the reduction of Hedgehog pathway signaling was observed. At the same concentration of 10 μM, GANT 58 treatment (2 ~ 3 days) also reduced Gli1 mRNA levels, which is indicative of strong pathway inhibition. |
| Animal experiment:[1] | |
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Animal models |
Nude mice injected subcutaneously with GLI1-positive 22Rv1 prostate cancer cells |
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Dosage form |
50 mg/kg Once daily by subcutaneous injection for 18 days |
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Applications |
For human prostate cancer xenografts, GANT 58 treatment resulted in the inhibition of additional xenograft growth and limited the increase in tumor size. Meanwhile, GANT 58 strongly reduced the expression levels of the target gene PTCH. No adverse side effects (e.g. weight loss and ulcerations) were observed during the 18-day treatment time. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Lauth M, Bergström A, Shimokawa T, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proceedings of the National Academy of Sciences of the United States of America, 2007, 104(20): 8455-8460. |
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| 描述 | GANT58是GLI的拮抗剂，抑制GLI1诱导转录，IC 50值为5 μM。 | |||||
| 靶点 | GLI | |||||
| IC50 | 5 μM | |||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
