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VER 155008

VER 155008

Catalog Number:
L002369183APE
Mfr. No.:
APE-A4387
Price:
$236
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      • Overview

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          Background

          VER 155008 is a potent inhibitor of heat shock protein 70 (Hsp70) family of chaperones, which have been shown to contribute to cancer cell survival via anti-apoptotic functions, that inhibits Hsp70 (with the value of 50% inhibition concentration IC50 of 0.5 μM) as well as heat shock cognate 71 kDa protein (Hsc70) and 78 kDa glucose-regulated protein (Grp78) but to a lesser extent. X-ray crystallography analysis reveals that VER 155008 binds to the ATPase pocket of Hsp70 leading to the inhibition of the intrinsic ATPase activity of Hsp70. Study results also have demonstrated that VER 155008 induces cell proliferation and apoptosis in human cancer cell lines.

      • Properties
        • Alternative Name
          adenosine-derived inhibitor, VER155008, VER-155008; 4-[[(2R,3S,4R,5R)-5-[6-amino-8-[(3,4-dichlorophenyl)methylamino]purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxymethyl]benzonitrile
          CAS Number
          1134156-31-2
          Molecular Formula
          C25H23Cl2N7O4
          Molecular Weight
          556.4
          Appearance
          A solid
          Purity
          99.72%
          Solubility
          ≥27.8 mg/mL in DMSO; insoluble in H2O; ≥4.65 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Haiyang Yu, Shan Lu, et al. "TDP-43 and HSP70 phase separate into anisotropic, intranuclear liquid spherical annuli." bioRxiv. March 29, 2020.
          2. Marrugal á, Ferrer I, et al. "Impact of Heat Shock Protein 90 Inhibition on the Proteomic Profile of Lung Adenocarcinoma as Measured by Two-Dimensional Electrophoresis Coupled with Mass Spectrometry." Cells. 2019 Jul 31;8(8). pii: E806. PMID:31370342
          3. He XM, Liu L, et al. "HSC70 from Haemaphysalis flava (Acari: Ixodidae) exerts anticoagulation activity in vitro." Ticks Tick Borne Dis. 2018 Oct 17. pii: S1877-959X(18)30258-9. PMID:30366643
          4. Santarriaga S, Haver HN, et al. "SRCP1 Conveys Resistance to Polyglutamine Aggregation." Mol Cell. 2018 Jul 19;71(2):216-228.e7. PMID:30029002
          5. XiChuan Tanga, LiWei Tanb, et al. "Gold nanorods together with HSP inhibitor-VER-155008 micelles for colon cancer mild-temperature photothermal therapy." Acta Pharmaceutica Sinica B Available online 5 June 2018.
          6. Tang, Pei-Ciao, et al. "Proteomic identification of hair cell repair proteins in the model sea anemone Nematostella vectensis." Hearing research (2015). PMID:26183436

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