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LH1306 Sale

目录号 : GC45771

A PD-1/PD-L1 interaction inhibitor

LH1306 Chemical Structure

Cas No.:2182653-84-3

规格 价格 库存 购买数量
1mg
¥1,028.00
现货
5mg
¥4,625.00
现货
10mg
¥8,224.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 25 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 334 and 4,214 nM, respectively, in reporter assays).

|1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 protein-protein interaction. J. Med. Chem. 62(15), 7250-7263 (2019).

Chemical Properties

Cas No. 2182653-84-3 SDF
Canonical SMILES CC1=C(COC2=CC=C(CNCCNC(C)=O)C(OC)=N2)C=CC=C1C3=C(C)C(COC4=NC(OC)=C(CNCCNC(C)=O)C=C4)=CC=C3
分子式 C38H48N6O6 分子量 684.8
溶解度 DMF: 1mg/mL,DMSO: 0.25mg/mL 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 1.4603 mL 7.3014 mL 14.6028 mL
5 mM 0.2921 mL 1.4603 mL 2.9206 mL
10 mM 0.146 mL 0.7301 mL 1.4603 mL
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Research Update

Design, Synthesis, Evaluation, and Structural Studies of C2-Symmetric Small Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein-Protein Interaction

J Med Chem 2019 Aug 8;62(15):7250-7263.PMID:31298541DOI:10.1021/acs.jmedchem.9b00795

A series of C2-symmetric inhibitors was designed and evaluated for inhibitory activity against the programmed cell death-1/programmed death-ligand 1(PD-1/PD-L1) protein-protein interaction (PPI) in a homogenous time-resolved fluorescence (HTRF) assay and PD-1 signaling in cell-based coculture assays. C2-symmetric inhibitors 2a (LH1306) and 2b (LH1307) exhibited IC50 values of 25 and 3.0 nM, respectively, in the HTRF assay. While 2a was ∼3.8-fold more potent than previously reported inhibitor 1a, 2b could not be differentiated from 1b due to their high potency and the limit of our HTRF assay conditions. In one cell-based coculture PD-1 signaling assay, 2a and 2b were 8.2- and 2.8-fold more potent in inhibiting PD-1 signaling than 1a and 1b, respectively. NMR and X-ray cocrystal structural studies provided more structural insights into the interaction between 2b and PD-L1; 2b binds to PD-L1 at the PD-1 binding site and induces the formation of a more symmetrically arranged PD-L1 homodimer than that previously reported for other inhibitors.