VER 155008

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Description: Hsp70 inhibitor
Chemical Name: 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine
Purity: ≥98% (HPLC)
Datasheet
Citations (21)
Reviews (2)
Literature (1)

Biological Activity for VER 155008

VER 155008 is a 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).

Compound Libraries for VER 155008

VER 155008 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for VER 155008

M. Wt 556.4
Formula C25H23Cl2N7O4
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1134156-31-2
PubChem ID 25195348
InChI Key ZXGGCBQORXDVTE-UMCMBGNQSA-N
Smiles NC1=NC=NC2=C1N=C(NCC5=CC=C(Cl)C(Cl)=C5)N2[C@@H]3O[C@H](COCC4=CC=C(C#N)C=C4)[C@@H](O)[C@H]3O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for VER 155008

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.64 100

Preparing Stock Solutions for VER 155008

The following data is based on the product molecular weight 556.4. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.8 mL 8.99 mL 17.97 mL
5 mM 0.36 mL 1.8 mL 3.59 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets for VER 155008

Certificate of Analysis / Product Datasheet
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References for VER 155008

References are publications that support the biological activity of the product.

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

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

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


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Keywords: VER 155008, VER 155008 supplier, VER155008, HSP, 70, antagonist, HSP70, adenosine, derived, inhibitor, inhibitors, inhibits, heat, shock, protein, selective, Hsp90, Hsp70, 3803, Tocris Bioscience

21 Citations for VER 155008

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

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

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

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

Gleixner et al (2017) N-Acetyl-l-Cysteine Protects Astrocytes against Proteotoxicity without Recourse to Glutathione. Mol Pharmacol 92 564 PMID: 28830914

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

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

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

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

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

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

Ganguly et al (2017) Hsc70 chaperone activity is required for the cytosolic slow axonal transport of synapsin. J Cell Biol 216 2059 PMID: 28559423

Cavanaugh et al (2015) Combined inhibition of heat shock proteins 90 and 70 leads to simultaneous degradation of the oncogenic signaling proteins involved in muscle invasive bladder cancer. Oncotarget 6 39821 PMID: 26556859

Amy S et al (2021) The Hydroxyquinoline Analogue YUM70 Inhibits GRP78 to Induce ER Stress-Mediated Apoptosis in Pancreatic Cancer. Cancer Res 81 1883-1895 PMID: 33531374

John R et al (2021) Clathrin packets move in slow axonal transport and deliver functional payloads to synapses. Neuron 109 2884-2901.e7 PMID: 34534453

Chiaw et al (2019) Hsp70 and DNAJA2 limit CFTR levels through degradation. PLoS One 14 e0220984 PMID: 31408507

Truman et al (2015) Quantitative proteomics of the yeast Hsp70/Hsp90 interactomes during DNA damage reveal chaperone-dependent regulation of ribonucleotide reductase. J Proteomics 112 285 PMID: 25452130

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

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

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

Rinaldi et al (2019) Feedback inhibition of cAMP effector signaling by a chaperone-assisted ubiquitin system. Nat Commun 10 2572 PMID: 31189917

Jodi et al (2016) Targeting HSP70 and GRP78 in canine osteosarcoma cells in combination with doxorubicin chemotherapy. Cell Stress Chaperones 21 1065-1076 PMID: 27631331


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Reviews for VER 155008

Average Rating: 5 (Based on 2 Reviews.)

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Potent HSP70 attenuation, alternative for apoptozole..
By Eric Dyne on 01/02/2021
Species: Human
Cell Line/Tissue: Microglia

Used this and apoptozole to knock down HSP70 expression. We ended up using Apoptozole for our work but this also worked well. Easy to reconstitute and found to be stable. Confirmed K.D. using qPCR, WB, and IF.

Cytotoxic to microglia at higher dosages (>1uM) observed using a cell viability assay and cell imaging.

review image

VER 155008 induces PARP cleavage in U2OS cells.
By Anonymous on 03/25/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma

Human osteosarcoma, U2OS, cells were incubated with VER 155008 (1 microM) for 24 h to follow PARP cleavage using Western blot. Hsp70 inhibition with VER 155008 significantly induced PARP cleavage in U2OS cells.

review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:

  • Cell Cycle and Mitosis
  • DNA Damage Repair
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  • Ubiquitin Proteasome Pathway
  • Chemotherapy Targets