VER-155008

Modify Date: 2024-01-03 23:04:57

VER-155008 structure	Common Name	VER-155008
	CAS Number	1134156-31-2	Molecular Weight	556.401
	Density	1.6±0.1 g/cm3	Boiling Point	856.3±75.0 °C at 760 mmHg
	Molecular Formula	C₂₅H₂₃Cl₂N₇O₄	Melting Point	N/A
	MSDS	USA	Flash Point	471.7±37.1 °C

Use of VER-155008

VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.

Name	5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine
Synonym	More Synonyms

Description	VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Cell Cycle/DNA Damage >> HSP Signaling Pathways >> Metabolic Enzyme/Protease >> HSP Research Areas >> Neurological Disease
Target	HSP70:0.5 μM (IC50) HSC70:2.6 μM (IC50) Grp78:2.6 μM (IC50)
In Vitro	VER-155008 is an inhibitor of Hsc70 and Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, a with a Kd of 0.3 μM for Hsp70, but shows no activities against Hsp90, with an IC50 of >200 μM. VER-155008 inhibits the proliferation of a variety of human colon and breast tumor cell lines, such as BT474, MB-468, HCT116 and HT29 cells, with GI50s of 10.4 μM, 14.4 μM, 5.3 μM, and 12.8 μM, respectively. VER-155008 (5-40 μM) induces client protein degradation in HCT116 and BT474 carcinoma cells. VER-155008 also induces apoptosis in human tumor cell lines[1]. VER-155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons[2]. VER-155008 (10 μM or 25 μM) inhibits Hsp70 and suppresses the proliferation of LNCaP95 cells. VER-155008 also reduces full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7) protein expression[3].
In Vivo	VER-155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice[1]. VER-155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice[2].
Cell Assay	Embryos are removed from a pregnant ddY mouse at 14 days of gestation. Cells are treated with or without 10 μM Aβ25-35 for 3 days, followed by the addition of 0.05, 0.5, or 5 μM VER-155008 or vehicle solution (0.1% DMSO) for 4 days. The Aβ25-35 is incubated at 37°C for 4 days prior to treatment to facilitate aggregation. The cells are fixed with 4% paraformaldehyde and immunostained at 4°C for 24 h with antibodies against the axonal marker, mouse phosphorylated neurofilament heavy subunit, and against the neuronal marker, rabbit microtubule-associated protein 2. Alexa Fluor 488-conjugated goat anti-mouse IgG (1:400) and Alexa Fluor 568-conjugated goat anti-rabbit IgG (1:400) are used as secondary antibodies. Fluorescence images (864.98 μm × 645.62 μm) are captured using a fluorescence microscopy system. The lengths of the pNF-H-positive axons are measured using MetaMorph version 7.8[2].
Animal Admin	Female BALB/c mice are dosed intravenously with 25 mg/kg VER-155008 into the lateral tail vein as a solution in 10% DMSO/5% Tween 80/85% saline (v/v/v). Animals are sacrificed at 5, 15 and 30 min, 1, 2, 4 and 6 h post dose[1].
References	[1]. Massey AJ, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. [2]. 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. [3]. 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.

Density	1.6±0.1 g/cm3
Boiling Point	856.3±75.0 °C at 760 mmHg
Molecular Formula	C₂₅H₂₃Cl₂N₇O₄
Molecular Weight	556.401
Flash Point	471.7±37.1 °C
Exact Mass	555.118835
PSA	164.36000
LogP	2.71
Vapour Pressure	0.0±0.3 mmHg at 25°C
Index of Refraction	1.748
Storage condition	-20℃

VER-155008 MSDS(Chinese)

RIDADR	NONH for all modes of transport
HS Code	2934999090

N/A

CAS#:1134156-55-0

~58%

VER-155008

CAS#:1134156-31-2

Literature: Williamson, Douglas S.; Borgognoni, Jenifer; Clay, Alexandra; Daniels, Zoe; Dokurno, Pawel; Drysdale, Martin J.; Foloppe, Nicolas; Francis, Geraint L.; Graham, Christopher J.; Howes, Rob; Macias, Alba T.; Murray, James B.; Parsons, Rachel; Shaw, Terry; Surgenor, Allan E.; Terry, Lindsey; Wang, Yikang; Wood, Mike; Massey, Andrew J. Journal of Medicinal Chemistry, 2009 , vol. 52, # 6 p. 1510 - 1513

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

5'-O-(4-Cyanobenzyl)-8-[(3,4-dichlorobenzyl)amino]adenosine

4-[[(2R,3S,4R,5R)-5-[6-amino-8-[(3,4-dichlorophenyl)methylamino]purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxymethyl]benzonitrile

Adenosine, 5'-O-[(4-cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-

VER-155008

DC Chemicals Limited
China
Product Name: VER155008
Price: $500.0/100mg $900.0/250mg $1800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 5'-O-[(4-CYANOPHENYL)METHYL]-8-[[(3,4-DICHLOROPHENYL)METHYL]AMINO]-ADENOSINE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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VER-155008

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