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VER-155008

Catalog No. T7010 CAS 1134156-31-2

Synonyms: VER155008

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, <100-fold selectivity over HSP90.

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VER-155008, CAS 1134156-31-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 85.00
25 mg	In stock	$ 166.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 492.00
200 mg	In stock	$ 688.00
1 mL * 10 mM (in DMSO)	In stock	$ 77.00

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Purity: 99.55%

Purity: 98.88%

Biological Description

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Storage & Solubility Information

Description	VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.
Targets&IC50	HSC70:2.6 μM, HSP70:0.5 μM, GRP78:2.6 μM
In vitro	VER-155008 inhibits the proliferation of human breast and colon cancer cell lines BT474, MB-468, HCT116, and HT29 with GI50s in the range 5.3-14.4 μM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells.[1] In the 8505C and FRO cells, VER-155008 reduces the cell viability and elevates the percentage of dead cells in a time- and dose- dependent manner.[2] VER-155008 causes a dose-dependent inhibition of cytokine-dependent AML cell proliferation.[3] VER-155008?shows an effective inhibition of cell proliferation in A549 and H1975 cells. [4]
In vivo	In HCT116 tumor bearing mice, VER-155008 (25 or 40 mg/kg, i.v.) demonstrates rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level.[1]
Kinase Assay	Hsc70, Hsp70 and Grp78 ?uorescence polarisation (FP) assay: The FP assay for Hsp70 is conducted in aqueous buffer consisting of 100 mM Tris pH 7.4, 150 mM KCl and 5 mM CaCl2, in a final assay volume of 100 μl, using 96 well black polystyrene high bind plates with a Fusion plate reader. N6-(6-amino)hexyl-ATP-5-FAM and the in-house protein preparation of GST-HSP70 3-382 have final concentrations in the assay of 20 nM and 400 nM, respectively. Compounds are tested as 10-point IC50s, with a final DMSO concentration of 5%. Assay mixtures are incubated for 3 h prior to reading on the Fusion (ex 485 nm; em 535 nm). The data is fitted using a 4 parameter logistical data model by XLFit 4. The FP assay for Hsc70 and Grp78 is carried out as described for Hsp70 using the same N6 -(6-amino)hexyl-ATP-5-FAM as the FP probe with the following modi?cations. For Hsc70, the protein and probe concentrations are 0.3 μM and 20 nM, respectively with a 30 min incubation at 22℃ while for Grp78, the protein and probe concentrations are 2 μM and 10 nM, respectively with a 2 h incubation at 22℃. The KD for the FAM-ATP probe was 0.24 μM for Hsc70 and 2 μM for Grp78.
Cell Research	All cell lines are grown in DMEM/10% FCS with GlutaMAX-I in a humidified atmosphere of 5% CO2 in air. Cell proliferation is determined using the sulforhodamine B (SRB) assay.(Only for Reference)

Synonyms	VER155008
Molecular Weight	556.4
Formula	C25H23Cl2N7O4
CAS No.	1134156-31-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55.6 mg/mL (100 mM)

References and Literature

1. Massey AJ, et al. Cancer Chemother Pharmacol. 2010, 66(3), 535-545. 2. Kim SH, et al. Biochem Biophys Res Commun. 2014, 454(1), 36-41. 3. Reikvam H, et al. Expert Opin Incestiq Drugs. 2013, 22(5), 551-563. 4. Wen W, et al. Exp Biol Med (Maywood). 2014, 239(5), 638-645. 5. Williamson DS, et al. J Med Chem. 2009, 52(6), 1510-1513. 6. Yang X, et al. Heat Shock Cognate 70 Inhibitor, VER-155008, Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimer's Disease. Front Pharmacol. 2018 Jan 30;9:48. 7. Kita K, et al. Heat shock protein 70 inhibitors suppress androgen receptor expression in LNCaP95 prostate cancer cells. Cancer Sci. 2017 Sep;108(9):1820-1827.

Citations

1. Du Y, Chen Z, Yan P, et al. Arginine–Arginine–Leucine Peptide Targeting Heat Shock Protein 70 for Cancer Imaging. Molecular Pharmaceutics. 2021 2. Wang J, Zhang J, Guo Z, et al.Targeting HSP70 chaperones by rhein sensitizes liver cancer to artemisinin derivatives.Phytomedicine.2023: 155156.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library GPCR Compound Library Inhibitor Library ReFRAME Related Library Cuproptosis Compound Library Bioactive Compounds Library Max CNS-Penetrant Compound Library Anti-Aging Compound Library Nucleotide Compound Library Anti-Cancer Compound Library

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Keywords

VER-155008 1134156-31-2 Autophagy Cytoskeletal Signaling Endocrinology/Hormones GPCR/G Protein Metabolism GPR HSP Heat shock proteins inhibit Inhibitor VER155008 VER 155008 inhibitor

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