VER-82576 NEW
| Price | $38 | $54 | $85 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: VER-82576 | CAS No.: 847559-80-2 |
| Purity: 99.16% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | VER-82576 |
| Description | VER-82576 (NVP-BEP800), a synthetic HSP90β inhibitor (IC50: 58 nM), exhibits >70-fold selectivity against Hsp90 family members Trap-1 and Grp94. |
| Cell Research | Cells are exposed to NVP-BEP800 for 24 hours. Cell proliferation is determined using either sulforhodamine B for adherent cells or MTS assay for suspension cells or those showing low adherence. Cell death is determined using a ToxiLight nondestructive cytotoxicity bioassay kit. Cell cycle progression is determined by RNase A/propidium iodide staining following fixation in 70% ethanol. Caspase-3/7 activity is determined using a homogeneous caspase activity kit.(Only for Reference) |
| Kinase Assay | Competitive binding fluorescent polarization assay: Recombinant Hsp90β, TAMRA-radicicol, or various concentrations of NVP-BEP800 is added in assay buffer (50 mM TRIS pH 7.4, 5 mM MgCl2, 150 mM KCl, and 0.1% CHAPS), mixed, and incubated at room temperature for 30 to 45 minutes prior to reading. The 2D-FIDA-based HTS assay based on confocal technologies monitors the decreased fluorescence polarization on displacement of the high affinity ligand TAMRA-radicicol from Hsp90β by NVP-BEP800. The concentration of NVP-BEP800 which inhibits Hsp90β by 50% is determined from the competition curve. |
| In vitro | In the A375 malignant melanoma transplantation tumor model, NVP-BEP800 (15 or 30 mg/kg/day, p.o.) treatment for 15 days dose-dependently decreased the levels of B-Raf and Akt phosphorylation and showed anticancer activity, with T/C values of 53% and 6% with NVP-BEP800 (15 and 30 mg/kg/day) treatment and almost total tumor inhibition with 30 mg/kg/day. 30 mg/kg inhibited almost all tumors. In BT-474 breast cancer transplantation tumors, NVP-BEP800 treatment increased the dissociation of Hsp90-p23 complex and decreased the levels of stable ErbB2, p-Akt and p-S6 in a dose-dependent manner, and NVP-BEP800 (30 mg/kg/day) treatment resulted in 38% tumor regression. Treatment with 15 mg/kg/day resulted in a T/C of 36%. |
| In vivo | NVP-BEP800 effectively inhibited the proliferation of various tumor cell lines including A375 cells (GI50: 38 nM) and PC3 cells (GI50: 1.05 μM). In A2058 and A549 cells, NVP-BEP800 (5-fold of GI50) increased the G2-M phase percentage. In BT-474 cells, NVP-BEP800 induced Akt and ErbB2 dephosphorylation, ErbB2 degradation, and Hsp70 induction in a concentration-dependent manner (IC50: 218/39.5/137/207 nM).At a concentration of 10 μM of Hsp70, the effects of NVP-BEP800 on the closely related GHKL ATPase, topoisomerase II, and structurally unrelated ATPases were observed. II and structurally unrelated ATPases were not significantly inhibited. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 1 mg/mL |
| Keywords | HSP | NVP-BEP 800 | Heat shock proteins | VER 82576 | NVP-BEP-800 | VER82576 | VER-82576 | Inhibitor | inhibit |
| Inhibitors Related | Ethoxyquin | SNX0723 | Tamoxifen | DN401 | SNX2112 | Ganetespib | Teprenone | Elesclomol | Rifabutin | Palmitic acid | Paeoniflorin | Tamoxifen Citrate |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Hematonosis Compound Library | Anti-Breast Cancer Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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