1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-L1-IN-9

PD-L1-IN-9 是一种 PD-L1 抑制剂,IC50 为 110.85 nM。PD-L1-IN-9 对人源 PD-L1Kd 为 319 nM,对鼠源 PD-L1Kd 为 450 nM。PD-L1-IN-9 可阻断 PD-1/PD-L1 相互作用,恢复 T 细胞介导的抗肿瘤免疫,诱导肿瘤组织中 PD-L1 降解。PD-L1-IN-9 具有抗肿瘤的活性,可用于黑色素瘤等肿瘤的研究。

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PD-L1-IN-9

PD-L1-IN-9 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PD-L1-IN-9 is a PD-L1 inhibitor with an IC50 of 110.85 nM. PD-L1-IN-9 has a Kd of 319 nM for human PD-L1 and a Kd of 450 nM for murine PD-L1. PD-L1-IN-9 blocks the PD-1/PD-L1 interaction, restores T cell-mediated anti-tumor immunity, and induces PD-L1 degradation in tumor tissues. PD-L1-IN-9 exhibits anti-tumor activity and can be used in the research of tumors such as melanoma[1].

体外研究
(In Vitro)

PD-L1-IN-9 (Compound Z38) (48 h) 对 B16-F10、Jurkat、HepG2、HCT116 和 HeLa 细胞系的细胞毒性较低,其 IC50 值范围为 28.18 μM 至 > 40 μM[1]
PD-L1-IN-9 (1.5625-25 μM;48 h) 可在 HepG2/Jurkat 共培养体系中通过重新激活 T 细胞,以剂量依赖的方式诱导 HepG2 细胞死亡[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: HepG2/Jurkat T cell coculture system
Concentration: 1.5625, 3.125, 6.25, 12.5 and 25 μM
Incubation Time: 48 h
Result: Promoted dose-dependent death of HepG2 cells, reducing HepG2 cell viability to 75.26% at 25 μM by reactivating Jurkat T cells to mediate killing.
体内研究
(In Vivo)

PD-L1-IN-9 (Compound Z38) (15-30 mg/kg;腹腔注射;7 天) 在荷 B16-F10 黑色素瘤小鼠中以剂量依赖的方式抑制肿瘤生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 6 weeks old, melanoma model via subcutaneous injection of B16-F10 cells)[1]
Dosage: 15, 30 mg/kg
Administration: i.p.; daily; 7 consecutive days
Result: Achieved 34% tumor growth inhibition rate (TGI), increased tumor-infiltrating CD4⁺ T cells to 14.9% and CD8⁺ T cells to 22.4%, and induced ~49% PD-L1 degradation in tumor tissues at 15 mg/kg.
Achieved 60% TGI, increased tumor-infiltrating CD4⁺ T cells to 19.3% and CD8⁺ T cells to 26.6%, and induced ~51% PD-L1 degradation in tumor tissues at 30 mg/kg.
分子量

483.56

Formula

C29H29N3O4

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.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PD-L1-IN-9
目录号:
HY-181096
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