2. PROTAC Immunology/Inflammation Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Hsp-targeting Chimeras LYTACs PD-1/PD-L1 HSP
  4. Hsp70TAC PD-1 Degrader-2

Hsp70TAC PD-1 Degrader-2 是一种 PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) 降解剂，其 Kd 值为 0.36 μM。Hsp70TAC PD-1 Degrader-2 可与 Hsp70 和 PD-L1 形成三元复合物，从而驱动 PD-L1 降解。Hsp70TAC PD-1 Degrader-2 以依赖 Hsp70 的方式，并通过小窝蛋白介导的内吞作用和溶酶体运输，诱导成熟膜结合型 PD-L1 降解。Hsp70TAC PD-1 Degrader-2 优先在 Hsp70 表达水平升高的肿瘤细胞中积累，实现肿瘤选择性 PD-L1 降解。Hsp70TAC PD-1 Degrader-2 可用于癌症研究，例如浸润性乳腺癌、多形性胶质母细胞瘤、弥漫性大 B 细胞淋巴瘤。(粉色: PD-1/PD-L1 配体 (HY-19745A)；蓝色: Hsp70 配体 (HY-182979)；黑色: 连接子 (HY-182982))。

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Hsp70TAC PD-1 Degrader-2

Hsp70TAC PD-1 Degrader-2 Chemical Structure

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Hsp70TAC PD-1 Degrader-2 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma[1]. (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).

IC50 & Target[1]

HSP70

4.18 μM (Kd)

体外研究
(In Vitro)

Hsp70TAC PD-1 Degrader-2 (Compound SP-2) (6.25-100 μM) 可与纯化的 Hsp70 结合，KD 值为 4.18 μM；还可与纯化的 PD-L1 结合，KD 值为 0.36 μM[1]。
Hsp70TAC PD-1 Degrader-2 (0.1-10 μM; 4-24 h) 可在 MDA-MB-231 细胞 (DC50 = 0.84 μM) 和 U-87 MG 细胞 (DC50 = 1.23 μM) 中诱导 PD-L1 呈时间和剂量依赖性降解[1]。
Hsp70TAC PD-1 Degrader-2 (1-5 μM; 24 h) 可有效降解 MDA-MB-231 细胞中成熟的膜结合型 PD-L1[1]。
Hsp70TAC PD-1 Degrader-2 (1 μM; 2-12 h) 可通过依赖溶酶体的途径诱导 MDA-MB-231 细胞中 PD-L1 的降解，该过程需要形成 PD-L1-SP-2-Hsp70 三元复合物[1]。
Hsp70TAC PD-1 Degrader-2 (1 μM; 12 h) 诱导的 MDA-MB-231 细胞中 PD-L1 降解依赖于 Hsp70 的表达以及小窝蛋白介导的内吞作用[1]。
Hsp70TAC PD-1 Degrader-2 (1-5 μM; 12 h) 可在过表达 Hsp70 的肿瘤细胞 (MDA-MB-231、U-87 MG、MCF-7、U937) 中选择性诱导 PD-L1 降解，但在低表达 Hsp70 的正常细胞 (HEK293T、MEF) 或 TE-1 细胞中无此作用[1]。

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

Hsp70TAC PD-1 Degrader-2 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 (triple-negative breast cancer), U-87 MG (glioblastoma multiforme)
Concentration: 0.1, 0.5, 1, 5, 10 μM
Incubation Time: 4, 8, 12, 24 h
Result: Induced time-dependent PD-L1 degradation starting at 8 h, with >80% depletion achieved at 24 h in both cell lines.
Yielded dose-dependent degradation with DC50 values of 0.84 μM in MDA-MB-231 cells and 1.23 μM in U-87 MG cells, with no observed "hook effect" at high concentrations.

Immunofluorescence[1]

Cell Line: MDA-MB-231
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: Reduced cell surface PD-L1 fluorescence signal as shown by immunofluorescence.
Confirmed a significant reduction in PD-L1-positive cells after treatment with 1 μM SP-2 for 24 h, compared to the DMSO control via flow cytometry.
分子量

950.24

Formula

C56H67N7O5S
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

Hsp70TAC PD-1 Degrader-2 相关分类

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  • 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.

Keywords:

Hsp70TAC PD-1 Degrader-2Hsp-targeting ChimerasLYTACsPD-1/PD-L1HSPHspTACsLysosome-targeting chimerasPD-1/Programmed death-ligand 1Heat shock proteinsternary complexlysosomal traffickingMDA-MB-231 cellsdiffuse large b-cell lymphomaU-87 MG cellscaveolin-mediated endocytosisbreast invasive carcinomaglioblastoma multiformeHsp70PD-L1Inhibitorinhibitorinhibit

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目录号：
HY-182959
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