1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Autophagy
  2. HSP
    Autophagy

VER-155008 

Cat. No.: HY-10941 Purity: 99.64%
Handling Instructions

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.

For research use only. We do not sell to patients.

VER-155008 Chemical Structure

VER-155008 Chemical Structure

CAS No. : 1134156-31-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 336 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1]

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.7973 mL 8.9863 mL 17.9727 mL
5 mM 0.3595 mL 1.7973 mL 3.5945 mL
10 mM 0.1797 mL 0.8986 mL 1.7973 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

VER-155008 is dissolved in 0.1% DMSO.

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

VER-155008 is dissolved in 10% DMSO/5% Tween 80/85% saline (v/v/v).

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

556.4

Formula

C₂₅H₂₃Cl₂N₇O₄

CAS No.

1134156-31-2

SMILES

O[[email protected]@H]([[email protected]]([[email protected]](N1C(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C1N=CN=C3N)O4)O)[[email protected]]4COCC5=CC=C(C#N)C=C5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 37 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.64%

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Product Name:
VER-155008
Cat. No.:
HY-10941
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