VER155008

製品コードS7751 バッチS775104

印刷

化学情報

Chemical Structure Synonyms Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H23Cl2N7O4
分子量 556.4 CAS No. 1134156-31-2
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 100 mg/mL (179.72 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
in vitro VER-155008 inhibits the proliferation of human breast and colon cancer cell lines BT474, MB-468, HCT116, and HT29 with GI50s in the range 5.3-14.4 μM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells.[1] In the 8505C and FRO cells, this compound reduces the cell viability and elevates the percentage of dead cells in a time- and dose- dependent manner.[2] It causes a dose-dependent inhibition of cytokine-dependent AML cell proliferation.[3] This chemical shows an effective inhibition of cell proliferation in A549 and H1975 cells. [4]
in vivo In HCT116 tumor bearing mice, VER-155008 (25 or 40 mg/kg, i.v.) demonstrates rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level.[1]

プロトコル(参考用のみ)

キナーゼアッセイ Hsc70, Hsp70 and Grp78 fluorescence polarisation (FP) assay
The FP assay for Hsp70 is conducted in aqueous buffer consisting of 100 mM Tris pH 7.4, 150 mM KCl and 5 mM CaCl2, in a final assay volume of 100 µl, using 96 well black polystyrene high bind plates with a Fusion plate reader. N6-(6-amino)hexyl-ATP-5-FAM and the in-house protein preparation of GST-HSP70 3-382 have final concentrations in the assay of 20 nM and 400 nM, respectively. Compounds are tested as 10-point IC50s, with a final DMSO concentration of 5%. Assay mixtures are incubated for 3 h prior to reading on the Fusion (ex 485 nm; em 535 nm). The data is fitted using a 4 parameter logistical data model by XLFit 4. The FP assay for Hsc70 and Grp78 is carried out as described for Hsp70 using the same N6 -(6-amino)hexyl-ATP-5-FAM as the FP probe with the following modifications. For Hsc70, the protein and probe concentrations are 0.3 μM and 20 nM, respectively with a 30 min incubation at 22℃ while for Grp78, the protein and probe concentrations are 2 μM and 10 nM, respectively with a 2 h incubation at 22℃. The KD for the FAM-ATP probe was 0.24 μM for Hsc70 and 2 μM for Grp78.
細胞アッセイ 細胞株 BT474, MB-468, HCT116, and HT29 cells
濃度 50 μM
反応時間 72 h
実験の流れ All cell lines are grown in DMEM/10% FCS with GlutaMAX-I in a humidified atmosphere of 5% CO2 in air. Cell proliferation is determined using the sulforhodamine B (SRB) assay.
動物実験 動物モデル HCT116 tumor bearing
投薬量 40 mg/kg
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/20012863/
  • https://pubmed.ncbi.nlm.nih.gov/25450359/
  • https://pubmed.ncbi.nlm.nih.gov/23586877/
  • https://pubmed.ncbi.nlm.nih.gov/24676905/
  • https://pubmed.ncbi.nlm.nih.gov/19256508/

カスタマーフィードバック

, , Neuroscience, 2014, 281C:164-177.

Data from [Data independently produced by , , Antiviral Res, 2018, 150:39-46]

Data from [Data independently produced by , , Cell Signal, 2017, 30:130-141]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A chaperone-proteasome-based fragmentation machinery is essential for aggrephagy [ Nat Cell Biol, 2025, 27(9):1448-1464] PubMed: 40866512
Pharmacological Modulation of the Unfolded Protein Response as a Therapeutic Approach in Cutaneous T-Cell Lymphoma [ Biomolecules, 2025, 15(1)76] PubMed: 39858470
USP8 and Hsp70 regulate endoreplication by synergistically promoting Fzr deubiquitination and stabilization [ Sci Adv, 2025, 11(12):eadq9111] PubMed: 40106570
Caspase-2 is a condensate-mediated deubiquitinase in protein quality control [ Nat Cell Biol, 2024, 26(11):1943-1957] PubMed: 39482354
Impairment of lipid homeostasis causes lysosomal accumulation of endogenous protein aggregates through ESCRT disruption [ Elife, 2024, 12RP86194] PubMed: 39713930
Small molecule inhibitor targeting the Hsp70-Bim protein-protein interaction in estrogen receptor-positive breast cancer overcomes tamoxifen resistance [ Breast Cancer Res, 2024, 26(1):33] PubMed: 38409088
Synergistic anticancer activity of HSP70 and HSF1 inhibitors in colorectal cancer cells: A new strategy for combination therapy [ Biochim Biophys Acta Mol Basis Dis, 2024, 1871(3):167630] PubMed: 39675530
Hsp70 Negatively Regulates Autophagy via Governing AMPK Activation, and Dual Hsp70-Autophagy Inhibition Induces Synergetic Cell Death in NSCLC Cells [ Int J Mol Sci, 2024, 25(16)9090] PubMed: 39201776
HSP70 positively regulates translation by interacting with the IRES and stabilizes the viral structural proteins VP1 and VP3 to facilitate duck hepatitis A virus type 1 replication [ Vet Res, 2024, 55(1):63] PubMed: 38760810
Bioinformatic Analysis of Actin-Binding Proteins in the Nucleolus During Heat Shock [ Genes (Basel), 2024, 15(12)1580] PubMed: 39766847

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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