Cart summary

You have no items in your shopping cart.

VER-155008

SKU: orb1226944

Description

A potent Hsp70 family (Hsc70/Hsp7/Grp78) inhibitor with Kd of 80 nM for Grp78; shows cellular activity in HCT116 cells (GI50= 5uM), has similar potencies in both Grp78 and Hsp70; inhibits the proliferation of human breast and colon cancer cell lines with GI50s of 5.3-14.4 uM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells; induced caspase-3/7 dependent apoptosis in BT474 cells.

Images & Validation

Key Properties

CAS Number1134156-31-2
MW556.4006
Purity>98% (HPLC)
FormulaC25H23Cl2N7O4
SMILESO[C@@H]([C@H]([C@H](N1C(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C(N=CN=C31)N)O4)O)[C@H]4COCC5=CC=C(C#N)C=C5
TargetHSP
SolubilityDMSO: ≥ 37 mg/mL

Bioactivity

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. 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.
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. VER-155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons. 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

VER-155008 | VER 155008 | VER155008

Similar Products

  • VER-155008 [orb1300147]

    99.55%

    1134156-31-2

    556.4

    C25H23Cl2N7O4

    10 mg, 25 mg, 100 mg, 5 mg, 2 mg, 50 mg, 1 ml x 10 mM (in DMSO), 200 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

VER-155008 (orb1226944)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

500 mg
2 mg
$ 80.00
5 mg
$ 110.00
10 mg
$ 140.00
25 mg
$ 240.00
50 mg
$ 410.00
100 mg
$ 660.00
200 mg
$ 910.00