Home / HSP70 Inhibitors / VER 155008

VER 155008

Catalog #: 3803
21 Citations Datasheet / COA / SDS
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3803/10
3803/50
VER 155008 | CAS No. 1134156-31-2 | HSP70 Inhibitors
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Description: Hsp70 inhibitor

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

Purity: ≥98%

Product Details
Citations (21)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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).

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

Background References

  1. Sequence-dependent internalization of aggregating peptides.
    Couceiro J, Gallardo R, De Smet F, De Baets G, Baatsen P, Annaert W, Roose K, Saelens X, Schymkowitz J, Rousseau F
    J Biol Chem, 2015;290(1):242-58.
  2. Dual regulation of SPI1/PU.1 transcription factor by heat shock factor 1 (HSF1) during macrophage differentiation of monocytes.
    Jego G, Lanneau D, de Thonel A, Berthenet K, Hazoume A, Droin N, Hamman A, Girodon F, Bellaye P, Wettstein G, Jacquel A, Duplomb L, Le Mouel A, Papanayotou C, Christians E, Bonniaud P, Lallemand-Mezger V, Solary E, Garrido C
    Leukemia, 2014;28(8):1676-86.
  3. Hsp70 Isoforms Are Essential for the Formation of Kaposi's Sarcoma-Associated Herpesvirus Replication and Transcription Compartments.
    Baquero-Perez B, Whitehouse A
    PLoS Pathog, 2015;11(11):e1005274.
  4. Mutation in integrin-linked kinase (ILK(R211A)) and heat-shock protein 70 comprise a broadly cardioprotective complex.
    Traister, Alexandr, Walsh, Mark, Aafaqi, Shabana, Lu, Minglian, Dai, Xiaojing, Henkleman, Mark R, Momen, Abdul, Zhou, Yu-Quing, Husain, Mansoor, Arab, Sara, Piran, Sara, Hannigan, Gregory, Coles, John G
    PLoS ONE, 2013;8(11):e77331.
  5. The Hsp90 machinery facilitates the transport of diphtheria toxin into human cells
    M Schuster, L Schnell, P Feigl, C Birkhofer, K Mohr, M Roeder, S Carle, S Langer, F Tippel, J Buchner, G Fischer, F Hausch, M Frick, C Schwan, K Aktories, C Schiene-Fi, H Barth
    Sci Rep, 2017;7(1):613.
  6. Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.
    Macias et al.
    J.Med.Chem., 2011;54:4034
  7. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells.
    Massey et al.
    Cancer Chemother.Pharmacol., 2009;66:535
  8. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.
    Williamson et al.
    J.Med.Chem., 2009;52:1510
  9. ATPases as drug targets: insights from heat shock proteins 70 and 90.
    Massey et al.
    J.Med.Chem., 2010;53:7280

Product Datasheets

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Citations for VER 155008

The citations listed below are publications that use Tocris products. Selected citations for VER 155008 include:

21 Citations: Showing 1 - 10

  1. The Hydroxyquinoline Analogue YUM70 Inhibits GRP78 to Induce ER Stress-Mediated Apoptosis in Pancreatic Cancer.
    Authors: Amy S Et al.
    Cancer Res  2021;81:1883-1895
  2. Clathrin packets move in slow axonal transport and deliver functional payloads to synapses.
    Authors: John R Et al.
    Neuron  2021;109:2884-2901.e7
  3. Hsp70 and DNAJA2 limit CFTR levels through degradation.
    Authors: Chiaw Et al.
    PLoS One  2019;14:e0220984
  4. Feedback inhibition of cAMP effector signaling by a chaperone-assisted ubiquitin system.
    Authors: Rinaldi Et al.
    Nat Commun  2019;10:2572
  5. N-Acetyl-l-Cysteine Protects Astrocytes against Proteotoxicity without Recourse to Glutathione.
    Authors: Gleixner Et al.
    Mol Pharmacol  2017;92:564
  6. Hsc70 chaperone activity is required for the cytosolic slow axonal transport of synapsin.
    Authors: Ganguly Et al.
    J Cell Biol  2017;216:2059
  7. Targeting HSP70 and GRP78 in canine osteosarcoma cells in combination with doxorubicin chemotherapy.
    Authors: Jodi Et al.
    Cell Stress Chaperones  2016;21:1065-1076
  8. Combined inhibition of heat shock proteins 90 and 70 leads to simultaneous degradation of the oncogenic signaling proteins involved in muscle invasive bladder cancer.
    Authors: Cavanaugh Et al.
    Oncotarget  2015;6:39821
  9. Oncogenic extracellular HSP70 disrupts the gap-junctional coupling between capillary cells.
    Authors: Thuringer Et al.
    J Cell Biol  2015;6:10267
  10. Sequence-dependent internalization of aggregating peptides.
    Authors: Couceiro Et al.
    Retrovirology  2015;290:242
  11. The regulation of TNFα production after heat and endotoxin stimulation is dependent on Annexin-A1 and HSP70.
    Authors: Nair Et al.
    Cell Stress Chaperones  2015;20:583
  12. Hsp72 is targeted to the mitotic spindle by Nek6 to promote K-fiber assembly and mitotic progression.
    Authors: O'Regan Et al.
    J Biol Chem  2015;209:349
  13. Hsp70 Isoforms Are Essential for the Formation of Kaposi's Sarcoma-Associated Herpesvirus Replication and Transcription Compartments.
    Authors: Baquero-Perez and Whitehouse
    PLoS Pathog  2015;11:e1005274
  14. A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90.
    Authors: Young Et al.
    Oncotarget  2015;11:113
  15. Quantitative proteomics of the yeast Hsp70/Hsp90 interactomes during DNA damage reveal chaperone-dependent regulation of ribonucleotide reductase.
    Authors: Truman Et al.
    J Proteomics  2015;112:285
  16. A cytosolic protein factor from the naked mole-rat activates proteasomes of other species and protects these from inhibition.
    Authors: Rodriguez Et al.
    Biochim Biophys Acta  2014;1842:2060
  17. Mutation in integrin-linked kinase (ILK(R211A)) and heat-shock protein 70 comprise a broadly cardioprotective complex.
    Authors: Traister Et al.
    PLoS One  2013;8:e77331
  18. The unfolded protein response selectively targets active smoothened mutants.
    Authors: Marada Et al.
    Mol Cell Biol  2013;33:2375
  19. Molecular mechanism of mutant p53 stabilization: the role of HSP70 and MDM2.
    Authors: Wiech Et al.
    PLoS One  2012;7:e51426
  20. The mammalian disaggregase machinery: Hsp110 synergizes with Hsp70 and Hsp40 to catalyze protein disaggregation and reactivation in a cell-free system.
    Authors: Shorter
    PLoS One  2011;6:e26319
  21. A unique role for heat shock protein 70 and its binding partner tissue transglutaminase in cancer cell migration.
    Authors: Boroughs Et al.
    J Biol Chem  2011;286:37094

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