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Submit ReviewPF 429242 dihydrochloride is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM). Also displays antiviral activity. Cell permeable.
Sold for research purposes under agreement from Pfizer Inc.
PF 429242 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 482.49 |
公式 | C25H35N3O2.2HCl |
储存 | Desiccate at RT |
纯度 | ≥97% (HPLC) |
CAS Number | 2248666-66-0 |
PubChem ID | 90488837 |
InChI Key | GSUZWFZKTIOWTI-MQWQBNKOSA-N |
Smiles | O=C(C2=CC=C(CN(CC)CC)C=C2)N(CCC3=CC=CC=C3OC)[C@@H]1CCNC1.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 24.12 | 50 | |
DMSO | 24.12 | 50 |
以下数据基于产品分子量 482.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.15 mL | 20.73 mL | 41.45 mL |
2.5 mM | 0.83 mL | 4.15 mL | 8.29 mL |
5 mM | 0.41 mL | 2.07 mL | 4.15 mL |
25 mM | 0.08 mL | 0.41 mL | 0.83 mL |
参考文献是支持产品生物活性的出版物。
Hay et al (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 17 4411 PMID: 17583500
Hawkins et al (2008) Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J.Pharmacol.Exp.Ther. 326 801 PMID: 18577702
Urata et al (2011) Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 85 795 PMID: 21068251
Olmstead (2012) Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents. PLoS.Pathog. 8 e1002468 PMID: 22241994
If you know of a relevant reference for PF 429242 dihydrochloride, please let us know.
关键词: PF 429242 dihydrochloride, PF 429242 dihydrochloride supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Other, Proteases, Non-selective, Antivirals, 3354, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 429242 dihydrochloride 的部分引用包括:
Flint et al (2019) A genome-wide CRISPR screen identifies N-acetylglucosamine-1-phosphate transferase as a potential antiviral target for Ebola virus. Nat Commun 10 285 PMID: 30655525
Kleinfelter et al (2015) Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion. Ann Rheum Dis 6 e00801 PMID: 26126854
Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193
Uchida et al (2016) Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation. Viruses 8 E46 PMID: 26875984
Tien et al (2019) Ambient particulate matter attenuates Sirtuin1 and augments SREBP1-PIR axis to induce human pulmonary fibroblast inflammation: molecular mechanism of microenvironment associated with COPD. Aging (Albany NY) 11 4654 PMID: 31299012
Urata et al (2015) Analysis of Assembly and Budding of Lujo Virus. J Virol 90 3257 PMID: 26719243
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