BMS-1001

Catalog No.S9610

For research use only.

BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction with EC50 of 253 nM. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.

BMS-1001 Chemical Structure

CAS No. 2113650-03-4

Purity & Quality Control

Choose Selective PD-1/PD-L1 Inhibitors

Biological Activity

Description BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction with EC50 of 253 nM. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.
Targets
PD-1/PD-L1 [1]
(Cell-free assay)
253 nM(EC50)
In vitro

BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is effective in attenuating the inhibitory effect of the cell surface-associated PD-L1.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: PD-L1+ aAPC/CHO-K1 cells (aAPCs), PD-1 Effector Cells (ECs)
  • Concentrations: 0.12 μM, 0.3 μM, 1.2 μM, 3 μM
  • Incubation Time: 24 h
  • Method:

    For the evaluation of the BMS impact on T cell inhibition by soluble PD-L1, the ECs are stimulated with the anti-CD3 antibody in the presence of the recombinant human sPD-L1. For this, the 96-well white flat bottom plates are coated overnight at 4°C with 5 μg/ml of the anti-CD3 antibody or the isotype control solution in PBS. The antibody solution is removed and the plates are washed 3 times with PBS and dried. sPD-L1 (aa 18–134) is diluted in PBS supplemented with the penicillin/streptomycin solution (100 U/ml final concentration each) in the presence of the BMS-1001 or a corresponding volume of DMSO. Then, 15 μl of the solution is added to each well of the antibodycoated plate. ECs are centrifuged and diluted to 50 000 per ml, and 60 μl of the cell solution is added to each well. The final concentration of sPD-L1 was 10 μg/ml (0.6 μM). The final concentrations of BMS-1001 are: 0.12, 0.3, 1.2 and 3 μM, giving the following BMS:sPD-L1 molar ratios: 1:5, 1:2, 2:1 and 5:1. The cells are cultured for 24 h and the luciferase activity assay is performed using the Bio-Glo Luciferase Assay System.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 594.65
Formula

C35H34N2O7

CAS No. 2113650-03-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C=C1OCC2=C(C(=CC=C2)C3=CC4=C(C=C3)OCCO4)C)OCC5=CC(=CC=C5)C#N)CNC(CO)C(=O)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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