VER-155008

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 Hsp70 家族 (Hsc70/Hsp7/Grp78) 抑制剂，对 Grp78 的 Kd 为 80 nM。

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.

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.

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.

VER-155008 | VER 155008 | VER155008

Cytoskeleton/Cell Adhesion Molecules

HSP

GRP78|HSC70|HSP70

Cancer

——

1134156-31-2

556.4006

C25H23Cl2N7O4

>98% (HPLC)

DMSO: ≥ 37 mg/mL

O[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

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

(-20℃)

With Ice Pack

≥ 2 years