Pifithrin-α hydrobromide CAS: 63208-82-2
MF: C16H18N2OS•HBr
MW: 367.30

Pifithrin-α hydrobromide (CAS 63208-82-2)

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备用名: Pifithrin-α hydrobromide is also known as PFT-α.
应用; Pifithrin-α hydrobromide is an inhibitor of p53 that reversibly blocks p53 dependent transcriptional activation and apoptosis.
CAS号码: 63208-82-2
纯度: ≥98%
分子量: 367.30
分子式: C16H18N2OS•HBr
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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Pifithrin-α hydrobromide is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. Pifithrin-α hydrobromide enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin (sc-280681), etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α hydrobromide protects mice from lethal genotoxic shock. Pifithrin-α protects mice from lethal whole body γ-irradiation, and does not induce visible tumors. Pifithrin-α hydrobromide protects against neuronal death in models of stroke and neurodegenerative disorders. Pifithrin-α is also an aryl hydrocarbon receptor (AHR) agonist, which leads to the upregulation of AHR target gene CYP1A1 (EC50 = 1.1 µM).


参考文献

1. Komarov, P G., et al., 1999. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science (New York, N.Y.). 285(5434): 1733-7. PMID: 10481009

2. Komarova, E A., et al., 2000. Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry. Biokhimia. 65(1): 41-8. PMID: 10702639

3. Culmsee, C., et al., 2001. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid beta-peptide. Journal of neurochemistry. 77(1): 220-8. PMID: 11279278

4. Lorenzo, Elisa., et al., 2002. Doxorubicin induces apoptosis and CD95 gene expression in human primary endothelial cells through a p53-dependent mechanism. The Journal of biological chemistry. 277(13): 10883-92. PMID: 11779855

5. Hoagland, Martin S., et al., 2005. The p53 inhibitor pifithrin-alpha is a potent agonist of the aryl hydrocarbon receptor. The Journal of pharmacology and experimental therapeutics. 314(2): 603-10. PMID: 15843497

6. Sohn, D., et al., 2009. Pifithrin-alpha protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53. Cell death and differentiation. 16(6): 869-78. PMID: 19229248

物理状态 :
Solid
溶解度 :
Soluble in DMSO (20 mg/ml), water, DMF (~1 mg/ml), 1:10 DMSO:PBS (pH 7.2) (~ 0.1 mg/ml), 100% ethanol, and methanol. Sparingly soluble in aqueous buffers.
保存 :
Store at -20° C
熔点 :
192.1-192.5° C
IC50 :
CYP1A1 upregulation: EC5050 = 1.1 µM
pK值 :
pKb: 3.19 (Predicted)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
PubChem CID :
默克索引 :
14: 7421
MDL 号码 :
MFCD00417851
SMILES :
CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br

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PMID: # 33393086  Mamidi, MK.|Samsa, WE.|Bashur, LA.|Chen, Y.|Chan, R.|Lee, B.|Zhou, G.| et al. 2021. J Cell Physiol. 236: 5686-5697.

PMID: # 30723502  Saini, H. et al. 2019. J Oncol. 2019: 6164807.

PMID: # 29802837  Zhang, L.|Ma, L.|Yan, T.|Han, X.|Xu, J.|Xu, J.|Xu, X.| et al. 2018. Exp. Cell Res. 369: 226-233.

PMID: # 28608259  Qiu, M. et al. 2017. Cancer Chemother. Pharmacol. 80: 275-286.

PMID: # 28102324  Lv, Y.|Zheng, J.|Zhou, Q.|Jia, L.|Wang, C.|Liu, N.|Zhao, H.|Ji, H.|Li, B.|Cao, W.| et al. 2017. Sci Rep. 7: 40967.

PMID: # 26804169  Kawatsuki, A.|Yasunaga, JI.|Mitobe, Y.|Green, PL.|Matsuoka, M.| et al. 2016. Oncogene. 35: 4509-17.

PMID: # 26647830  Eleftheriadis, T.|Pissas, G.|Antoniadi, G.|Tsogka, K.|Sounidaki, M.|Liakopoulos, V.|Stefanidis, I.| et al. 2016. Mol Med Rep. 13: 925-32.

PMID: # 26884717  Yu, W. et al. 2016. Int. J. Biol. Sci. 12: 198-209.

PMID: # 26431790  Yin, R. et al. 2016. Respir Physiol Neurobiol. 220: 81-7.

PMID: # 27121748  Park, GB.|Park, SH.|Kim, D.|Kim, YS.|Yoon, SH.|Hur, DY.| et al. 2016. Int. J. Oncol. 49: 411-21.

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