SAG
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SAG是合成的含有氯噻吩的Hh途径激动剂,调节smo活性.SAG是SMO激动剂,EC50为3 nM,但抑制Hedgehog信号的EC50大于1 μM[1].
Smoothened (SMO)是GPCR样受体,介导hedgehog信号,通过Gli转录因子,与Patched蛋白共同调节基因表达,对于胚胎发育和成人组织稳态具有重要作用.
在小鼠细胞培养实验中(Shh-LIGHT2),SAG诱导通路活化,EC50约为3 nM.它在通路中的活性有所不同,SAG浓度超过1 μM时,通路活性显著降低[1].SAG与SMO七螺旋束直接结合.SAG剂量依赖性地阻断该关联,SAG/SMO复合体的表观解离常数(KD)为59 nM[2].
在CGNP P4野生型小鼠原代培养物中,SAG拮抗GC的抗增殖作用.15-240 nM的SAG抑制糖皮质激素的神经毒性作用,而不干扰糖皮质激素对肺成熟的的有益作用[2].
参考文献:
1. Chen JK, Taipale J, Young KE et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.
2. Heine VM, Griveau A, Chapin C et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. Sci Transl Med. 2011 Oct 19;3(105):105ra104.
Storage | Store at -20°C |
M.Wt | 490.06 |
Cas No. | 912545-86-9 |
Formula | C28H28ClN3OS |
Solubility | ≥24.5 mg/mL in DMSO; ≥16.33 mg/mL in H2O with gentle warming and ultrasonic; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN[C@@]1([H])CC[C@@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1 |
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。 |
细胞实验[1]: | |
细胞系 |
Shh-LIGHT细胞系 |
溶解方法 |
在DMSO中的溶解度> 24.5mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
0.1~100 μM |
应用 |
SAG诱导小鼠培养细胞中的Hh通路活化,EC50为3nM。但是,当SAG浓度超过1μM时,通路活性显著降低。 |
动物实验[2]: | |
动物模型 |
P4野生型小鼠 |
剂量 |
SAG(20μg/g),泼尼松龙(0.67μg/g),7日,每日一次 |
应用 |
SAG在治疗剂量下可有效预防糖皮质激素引起的小鼠新生儿小脑发育异常。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Chen JK, Taipale J, Young KE et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. [2] Heine VM, Griveau A, Chapin C et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. Sci Transl Med. 2011 Oct 19;3(105):105ra104. |
质量控制和MSDS
- 批次:
化学结构
![SAG](http://www.apexbt.com/media/diy/images/struct/B5837.png)