BMS-1

Catalog No.S7911 Batch:S791103

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Technical Data

Formula

C29H33NO5
Molecular Weight 475.58 CAS No. 1675201-83-8
Solubility (25°C)* In vitro DMSO 95 mg/mL (199.75 mM)
Water 95 mg/mL (199.75 mM)
Ethanol 5 mg/mL (10.51 mM)
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description BMS-1 is a small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of 6 nM.
Targets
PD-1/PD-L1 interaction [1]
(Cell-free assay)
0.006 μM
In vitro

PD-1/PD-L1 inhibitor 1 causes half-reduced cell viability at lower concentrations in triple-negative breast cancer (TNBC), activates ERK in MDA-MB-231 and MCF7, significantly increases IL-8 expression in MDA-MB-231 and HCC1806 when administrated in combination with ERK1/2 inhibitor, also potently downregulates the IL-8 expression to its half amount in MDA-MB-231.[2]
In vivo

PD-1/PD-L1 inhibitor 1 combined with Jiedu Sangen Decoction (JSD) remarkably inhibits and reverses epithelial-mesenchymal transition (EMT) via PI3K/AKT signaling pathway.[3]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    MDA-MB-231 cells, HCC1937 cells, HCC1806 cells, MCF7 cells

  • Concentrations

    --

  • Incubation Time

    72 h

  • Method

    Cell proliferation is determined by the MTS assay. A total of 1-2×103 cells are plated in 100 μl medium in each well of a 96-well plate. After 24 h, PD-1/PD-L1 inhibitor 1 and ERK1/2 inhibitor are diluted to the desired concentrations in test medium (DMEM containing 1% fetal bovine serum) and added as single or as combined treatment in triplicate for 72 h.
Animal Study:

[3]
  • Animal Models

    Male specific pathogen free BALB/c mice of hepatic metastatic colorectal cancer (CRC) model

  • Dosages

    100 µg

  • Administration

    i.p.

Selleck's BMS-1 has been cited by 13 publications

Development and In Vivo Evaluation of Small-Molecule Ligands for Positron Emission Tomography of Immune Checkpoint Modulation Targeting Programmed Cell Death 1 Ligand 1 [ J Med Chem, 2024, 67(5):4036-4062] PubMed: 38442487
Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction [ Int. J. Mol. Sci, 2023, 24(4)] PubMed: None
Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction [ Int J Mol Sci, 2023, 24(4)3971] PubMed: 36835382
Identification of CBPA as a New Inhibitor of PD-1/PD-L1 Interaction [ Int J Mol Sci, 2023, 24(4)3971] PubMed: 36835382
Hepatobiliary Tumor Organoids Reveal HLA Class I Neoantigen Landscape and Antitumoral Activity of Neoantigen Peptide Enhanced with Immune Checkpoint Inhibitors [ Adv Sci (Weinh), 2022, 9(22):e2105810] PubMed: 35665491
Alpha5 nicotinic acetylcholine receptor mediated immune escape of lung adenocarcinoma via STAT3/Jab1-PD-L1 signalling [ Cell Commun Signal, 2022, 20(1):121] PubMed: 35971127
Discovery of a new inhibitor targeting PD-L1 for cancer immunotherapy [ Neoplasia, 2021, 23(3):281-293] PubMed: 33529880
Inhibitors of PD-1/PD-L1 and ERK1/2 impede the proliferation of receptor positive and triple-negative breast cancer cell lines [ J Cancer Res Clin Oncol, 2021, 10.1007/s00432-021-03694-4] PubMed: 34185141
The Stone Guest: How Does pH Affect Binding Properties of PD-1/PD-L1 Inhibitors [ ChemMedChem, 2021, 16(3):568-577] PubMed: 33085193
Small-molecule PD-L1 inhibitor BMS1166 abrogates the function of PD-L1 by blocking its ER export [ Oncoimmunology, 2020, 9(1):1831153] PubMed: 33110706

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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