An inhibitor of Hsp70, Hsc70, and GRP78
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VER-155008

Item No. 17257

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5'-O-[(4-cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine
CAS Number
1134156-31-2
Molecular Formula
C25H23Cl2N7O4
Formula Weight
556.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml
λmax
216, 275 nm
SMILES
O[C@H]1[C@@H](O)[C@H](N2C(NCC3=CC=C(Cl)C(Cl)=C3)=NC4=C2N=CN=C4N)O[C@@H]1COCC5=CC=C(C#N)C=C5
InChi Code
InChI=1S/C25H23Cl2N7O4/c26-16-6-5-15(7-17(16)27)9-30-25-33-19-22(29)31-12-32-23(19)34(25)24-21(36)20(35)18(38-24)11-37-10-14-3-1-13(8-28)2-4-14/h1-7,12,18,20-21,24,35-36H,9-11H2,(H,30,33)(H2,29,31,32)/t18-,20-,21-,24-/m1/s1
InChi Key
ZXGGCBQORXDVTE-UMCMBGNQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $194

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    25 mg

    $427

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    50 mg

    $801

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    Cayman Chemical
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    Product Description

    VER-155008 is an inhibitor of heat shock protein 70 (Hsp70), heat shock cognate 71 kDa protein (Hsc70), and glucose-regulated protein 78 kDa (GRP78), also known as heat shock 70 kDa protein 5 (HspA5) or immunoglobulin heavy chain-binding protein (BiP; IC50s = 0.5, 2.6, and 2.6 µM, respectively).1 It inhibits the ATPase activity of Hsp70 and is selective for Hsp70, Hsc70, and GRP78 over Hsp90 (IC50 = >200 µM). VER-155008 reduces proliferation of BT474 breast cancer, HCT116 colorectal cancer, and HT-29 colorectal cancer cells (GI50s = 10.4, 5.3, and 12.8 µM, respectively). It induces degradation of the Hsp90 client proteins HER2 and C-RAF in BT474 and HCT116 cells, apoptosis in HCT116 cells, and paraptosis in FRO and 8505C anaplastic thyroid carcinoma cells.1,2 VER-155008 reduces tumor volume in a PC12 pheochromocytoma mouse xenograft model and rescues memory deficits in a 5XFAD transgenic mouse model of Alzheimer’s disease.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Massey, A.J., Williamson, D.S., Browne, H., et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother. Pharmacol. 66(3), 535-545 (2015).

    2. Kim, S.H., Kang, J.G., Kim, C.S., et al. The hsp70 inhibitor VER155008 induces paraptosis requiring de novo protein synthesis in anaplastic thyroid carcinoma cells. Biochim. Biophys. Acta 454(1), 36-41 (2014).

    3. Xu, F., Lin, D., Jiang, W., et al. HSP70 inhibitor VER155008 suppresses pheochromocytoma cell and xenograft growth by inhibition of PI3K/AKT/mTOR and MEK/ERK pathways. Int. J. Clin 12(7), 2585-2594 (2019).

    4. Yang, X., and Tohda, C. Heat shock cognate 70 inhibitor, VER-155008, reduces memory deficits and axonal degeneration in a mouse model of Alzheimer’s disease. Front. Pharmacol. 9, 48 (2018).