Cyclic Pifithrin-α hydrobromide
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.
IC50:N/A
Pifithrin-α是一种p53抑制剂,阻断p53应答基因的p53依赖性转录激活。
化疗和放射疗法治疗癌症通常具有限制其疗效的严重副作用。P53决定抗癌治疗的毒副作用,因此可能是一种用于降低抗癌治疗过程中对正常组织损害的适当靶点[1]。因此,找到p53的抑制剂可能是用于减少癌症治疗和与p53诱导相关的其他类型应激的副作用的有效方法。
体外:在ConA细胞中,Pifithrin-α阻断p53应答基因的p53依赖性转录激活。Pifithrin-α(10μM)抑制由依托泊苷、紫杉醇、Dox、阿糖胞苷引导的C8细胞凋亡。Pifithrin-α对人二倍体成纤维细胞应答DNA损伤的p53依赖性生长停滞具有显著抑制效果,而对p53缺陷成纤维细胞无显著抑制。Pifithrin-α可以监测p53的入核转运或出核转运(或两者),或者可能引起核p53不稳定性[2]。
体内:在60%杀死剂量的γ辐射(8 Gy对于C57BL和6 Gy 对于Balb / c)处理的两株小鼠中,Pifithrin-α(2.2 mg/kg i.p.)处理的小鼠完全存活。Pfithrin-α预处理的小鼠比未接受Pifithrin-α预处理的辐射小鼠体重下降较少。小鼠全身γ辐射后,Pifithrinα(2.2 mg/kg)消除DNA复制的p53依赖性调节[2]。
临床试验:目前尚未进行临床研究。
参考文献:
[1] Komarova EA and Gudkov A V. Could p53 be A target for therapeutic suppression Semin. Cancer Biol. 1998, 8: 389-400.
[2] Komarov PG, Komarova EA, Kondratov RV, Christov-Tselkov K, Coon JS, Chernov MV, Gudkov AV. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science. 1999 Sep 10; 285(5434):1733-7.
Storage | Desiccate at RT |
M.Wt | 349.29 |
Cas No. | 511296-88-1 |
Formula | C16H16N2S·HBr |
Synonyms | Pifithrin-β |
Solubility | insoluble in H2O; ≥25 mg/mL in DMSO with gentle warming; ≥4.42 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole;hydrobromide |
SDF | Download SDF |
Canonical SMILES | CC1=CC=C(C=C1)C2=CN3C4=C(CCCC4)SC3=N2.Br |
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
- 批次: