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Submit ReviewVER 155008
说明： Hsp70 inhibitor
化学名： 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine
纯度： ≥98% (HPLC)
生物活性 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).
化合物库 for VER 155008
VER 155008 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for VER 155008
| 分子量 | 556.4 |
| 公式 | C25H23Cl2N7O4 |
| 储存 | Desiccate at RT |
| 纯度 | ≥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 |
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.
溶解性数据 for VER 155008
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 55.64 | 100 |
制备储备液 for VER 155008
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for VER 155008
参考文献 for VER 155008
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for VER 155008, please let us know.
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关键词: 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 篇 VER 155008 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VER 155008 的部分引用包括：
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
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
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
Ganguly et al (2017) Hsc70 chaperone activity is required for the cytosolic slow axonal transport of synapsin. J Cell Biol 216 2059 PMID: 28559423
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
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
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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Potent HSP70 attenuation, alternative for apoptozole..
By
Eric Dyne on 01/02/2021
种属： Human
细胞系/组织： 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.
VER 155008 induces PARP cleavage in U2OS cells.
By
Anonymous on 03/25/2019
分析类型： In Vitro
种属： Human
细胞系/组织： 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.
该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets