VER 155008

Cat. No. 3803

VER 155008 C25H23Cl2N7O4 [1134156-31-2]

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Chemical Name: 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine

Biological Activity

Novel adenosine-derived inhibitor of Heat Shock Protein 70 (Hsp70) (IC50 = 0.5 μM). Inhibits cell proliferation of multiple human tumor cell lines in vitro. Also binds Hsc70 and Grp78; displays selectivity against Hsp90β (IC50 >200 μM for Hsp90β).

Technical Data

M.Wt:
556.4
Formula:
C25H23Cl2N7O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
1134156-31-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Macias et al (2011) Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity. J.Med.Chem. 54 4034. PMID: 21526763.

Massey et al (2010) ATPases as drug targets: insights from heat shock proteins 70 and 90. J.Med.Chem. 53 7280. PMID: 20608738.

Massey et al (2009) A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother.Pharmacol. 66 535. PMID: 20012863.

Williamson et al (2009) Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. J.Med.Chem. 52 1510. PMID: 19256508.

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Citations are publications that use Tocris products. Selected citations for VER 155008 include:

Baquero-Perez and Whitehouse (2015) Hsp70 Isoforms Are Essential for the Formation of Kaposi's Sarcoma-Associated Herpesvirus Replication and Transcription Compartments. PLoS Pathog 11 e1005274. PMID: 26587836.

Couceiro et al (2015) Sequence-dependent internalization of aggregating peptides. Retrovirology 290 242. PMID: 25391649.

Nair et al (2015) The regulation of TNFα production after heat and endotoxin stimulation is dependent on Annexin-A1 and HSP70. Cell Stress Chaperones 20 583. PMID: 25753354.

O'Regan et al (2015) Hsp72 is targeted to the mitotic spindle by Nek6 to promote K-fiber assembly and mitotic progression. J Biol Chem 209 349. PMID: 25940345.

Thuringer et al (2015) Oncogenic extracellular HSP70 disrupts the gap-junctional coupling between capillary cells. J Cell Biol 6 10267. PMID: 25868858.

Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. Oncotarget 11 113. PMID: 25700737.

Rodriguez et al (2014) A cytosolic protein factor from the naked mole-rat activates proteasomes of other species and protects these from inhibition. Biochim Biophys Acta 1842 2060. PMID: 25018089.

Marada et al (2013) The unfolded protein response selectively targets active smoothened mutants. Mol Cell Biol 33 2375. PMID: 23572559.

Traister et al (2013) Mutation in integrin-linked kinase (ILK(R211A)) and heat-shock protein 70 comprise a broadly cardioprotective complex. PLoS One 8 e77331. PMID: 24260102.

Wiech et al (2012) Molecular mechanism of mutant p53 stabilization: the role of HSP70 and MDM2. PLoS One 7 e51426. PMID: 23251530.

Boroughs et al (2011) A unique role for heat shock protein 70 and its binding partner tissue transglutaminase in cancer cell migration. J Biol Chem 286 37094. PMID: 21896482.

Shorter (2011) The mammalian disaggregase machinery: Hsp110 synergizes with Hsp70 and Hsp40 to catalyze protein disaggregation and reactivation in a cell-free system. PLoS One 6 e26319. PMID: 22022600.

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Keywords: VER 155008, supplier, VER155008, HSP, 70, antagonist, HSP70, adenosine, derived, inhibitor, inhibitors, inhibits, heat, shock, protein, selective, Hsp90, Tocris Bioscience, Hsp70 Inhibitor products

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