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Name:VER-155008
| Chemical structure | Code NO. |
MT0552 |
 |
Name |
VER-155008 |
Synonym |
VER155008; VER 155008 | |
CAS NO. |
1134156-31-2 | |
Chemical Formula |
C25H23Cl2N7O4 | |
MW |
556.4 | |
Purity |
>98% | |
Solubility(R.T.: 25℃) |
DMSO:37mg/mL |
|
Stability |
- 20℃, 2 years |
Availability and price
Size
Price
Availability
100mg
$780
In stock
1g
$1800
In stock
>1g
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Quality Control: 1.VER155008-HNMR.pdf 2.VER155008-HPLC.pdf
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Description
VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 with GI50 of 5.3-14.4 uM in human breast and colon cancer cell lines.
IC50 value: 5.3-14.4 uM(GI50); 80 nM(Kd) [1] [2]
Target: Hsp70 inhibitor
in vitro: VER-155008 inhibited the proliferation of human breast and colon cancer cell lines with GI(50)s in the range 5.3-14.4 microM, and induced Hsp90 client protein degradation in both HCT116 and BT474 cells. As a single agent, VER-155008 induced caspase-3/7 dependent apoptosis in BT474 cells and non-caspase dependent cell death in HCT116 cells. VER-155008 potentiated the apoptotic potential of a small molecule Hsp90 inhibitor in HCT116 but not HT29 or MDA-MB-468 cells [1]. VER-155008 (HCT116 GI50 = 5 μM), has similar potencies in both Grp78 and Hsp70 [2]. Inhibition of Hsp70/Hsc70 activity with VER 155008 attenuated the protection afforded by N-acetyl cysteine in a dose-responsive manner [3].
in vivo: VER-155008 demonstrated rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level [1].
IC50 value: 5.3-14.4 uM(GI50); 80 nM(Kd) [1] [2]
Target: Hsp70 inhibitor
in vitro: VER-155008 inhibited the proliferation of human breast and colon cancer cell lines with GI(50)s in the range 5.3-14.4 microM, and induced Hsp90 client protein degradation in both HCT116 and BT474 cells. As a single agent, VER-155008 induced caspase-3/7 dependent apoptosis in BT474 cells and non-caspase dependent cell death in HCT116 cells. VER-155008 potentiated the apoptotic potential of a small molecule Hsp90 inhibitor in HCT116 but not HT29 or MDA-MB-468 cells [1]. VER-155008 (HCT116 GI50 = 5 μM), has similar potencies in both Grp78 and Hsp70 [2]. Inhibition of Hsp70/Hsc70 activity with VER 155008 attenuated the protection afforded by N-acetyl cysteine in a dose-responsive manner [3].
in vivo: VER-155008 demonstrated rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level [1].
References
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