SH-4-54
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.
SH-4-54是一种有效的STAT3抑制剂,对STAT3和STAT5的KD值分别为300和464 nM[1].
STAT3是属于STAT转录因子家族的一种转录因子.STAT3信号在脑肿瘤干细胞(BTSC)和胶质母细胞瘤(GBM)的存活和增殖中扮演重要角色[1].
SH-4-54是一种有效的STAT抑制剂.SH-4-54可抑制STAT3与磷酸肽的相互作用,Ki值为10-30 μM.SH-4-54对STAT3具有比STAT1强10倍多的选择性.SH-4-54可以浓度依赖的方式抑制pSTAT3(Y705),对pSTAT3(S727)无效果,表明SH-4-54结合STAT3 SH2结构域.另外,SH-4-54可降低pSTAT3水平,抑制参与细胞生长和存活的下游靶点细胞周期蛋白D1和Bcl-xL[1].
在小鼠中,腹腔注射SH-4-54(10 mg/kg)30 min后大脑中的浓度为700 nM.在105 BT73神经胶质瘤细胞异种移植NOD-SCID小鼠中,SH-4-54(10 mg/kg)可减少肿瘤细胞和pSTAT3表达.并且,SH-4-54可抑制增殖并诱导细胞凋亡[1].
参考文献:
[1]. Haftchenary S, Luchman HA, Jouk AO, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett, 2013, 4(11): 1102-1107.
- 1. Memarzadeh K, Savage DJ, et al. "Low UBE4B expression increases sensitivity of chemoresistant neuroblastoma cells to EGFR and STAT5 inhibition." Cancer Biol Ther. 2019 Sep 1:1-14. PMID:31475882
- 2. Litvinchuk A, Wan YW, et al. "Complement C3aR Inactivation Attenuates Tau Pathology and Reverses an Immune Network Deregulated in Tauopathy Models and Alzheimer's Disease." Neuron. 2018 Dec 19;100(6):1337-1353.e5. PMID:30415998
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 610.59 |
Cas No. | 1456632-40-8 |
Formula | C29H27F5N2O5S |
Solubility | insoluble in H2O; ≥20.25 mg/mL in DMSO; ≥24.2 mg/mL in EtOH |
SDF | Download SDF |
Canonical SMILES | FC(C(S(=O)(N(C)CC(N(C1=CC=C(C(O)=O)C=C1)CC2=CC=C(C=C2)C3CCCCC3)=O)=O)=C(C(F)=C4F)F)=C4F |
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。 |
质量控制和MSDS
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