BMS-8

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BMS-8 

BMS-8 抑制 PD-1/PD-L1 相互作用,其 IC50 值为 7.2 μM。BMS-8 直接与 PD-L1 结合,可诱导 PD-L1 同源二聚体的形成,从而阻止其与 PD-1 的相互作用。

BMS-8

BMS-8 Chemical Structure

CAS No. : 1675201-90-7

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生物活性

BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1[1].

体外研究
(In Vitro)

BMS-8 tends to have a more stable binding mode with one PD-L1 monomer than the other and the small-molecule inducing PD-L1 dimerization was further stabilized by the non-polar interaction of Ile54, Tyr56, Met115, Ala121, and Tyr123 on both monomers and the water bridges involved in ALys124[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

494.42

Formula

C27H28BrNO3

CAS 号

1675201-90-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Eun-Hye Kim, et al. Preparation of Biphenyl-Conjugated Bromotyrosine for Inhibition of PD-1/PD-L1 Immune Checkpoint Interactions. Int J Mol Sci. 2020 May 21;21(10):3639.

    [2]. Danfeng Shi, et al. Computational Insight Into the Small Molecule Intervening PD-L1 Dimerization and the Potential Structure-Activity Relationship. Front Chem. 2019 Nov 12;7:764.

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