2. PROTAC Immunology/Inflammation Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. LYTACs PD-1/PD-L1 HSP
  4. dPDL1-4

dPDL1-4 是一种强效且具有选择性的 eHSPTAC eHSP90 PD-L1 降解剂，其 DC50 为 7.77 μM (HeLa) 和 6.52 μM (B16F10)。dPDL1-4 可连接 eHSP90 与靶蛋白，诱导溶酶体降解。dPDL1-4 能显著降解 PD-L1，并抑制肿瘤生长。dPDL1-4 可用于宫颈癌和黑色素瘤的研究。((红色：eHSP90 配体 (HY-174476)；蓝色：PD-L1 配体 (HY-116274)；黑色：连接子 (HY-W021787)；HSP 配体 + linker: HY-174799))。

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dPDL1-4 Chemical Structure

dPDL1-4 Chemical Structure

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dPDL1-4 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

dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799))[1].

体外研究
(In Vitro)

dPDL1-4 (5-20 μM, 12-24 h) 以依赖于 eHSP90、三元复合物和溶酶体的方式促进 HeLa 和 B16F10 细胞膜上 PD-L1 的降解[1]。

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

dPDL1-4 相关抗体:

Western Blot Analysissup>[1]

Cell Line: HeLa and B16F10 cells
Concentration: 0, 1, 3, 5, 10, 20 μM
Incubation Time: 12 h
Result: Induced dose- and time-dependent degradation of PD-L1 in HeLa cells (Dmax = 68%) and B16F10 cells (Dmax = 56%).

Western Blot Analysissup>[1]

Cell Line: B16F10 cells
Concentration: 5 μM
Incubation Time: 12 h
Result: Inhibited the degradation of membrane-associated PD-L1 by BMS-8 (HY-116274) or HSP90i-Ac.

Western Blot Analysissup>[1]

Cell Line: HeLa cells
Concentration: 10, 20 μM
Incubation Time: 24 h
Result: Inhibited the degradation of membrane-associated PD-L1 by Bafilomycin A1 (HY-100558) and Monensin (HY-N4302) but not by MG132 (HY-13259).
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat 50 mg/kg i.v. AUC0-∞ 27866.1 μg/L·h
Rat 50 mg/kg i.v. T1/2 1.6 h
体内研究
(In Vivo)

dPDL1-4 (50 mg/kg, i.p., 每 2 天一次，共 6 剂) 在 B16F10 黑色素瘤小鼠模型中有效降解了 PD-L1并且显著地抑制了肿瘤生长[1]。

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

Animal Model: B16F10 melanoma syngeneic mouse model established by tumor-bearing mice (C57BL/6J, 6-7 weeks, female)[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection(i.p.), every 2 days for 6 doses.
Result: Suppressed tumor growth significantly, without causing notable weight loss.
Induced a remarkable decrease in the PD-L1 level among all the treatments.
Increased the percentage of activated cytotoxic T cells (CD8+cells).
分子量

1133.17

Formula

C60H74BrN7O10
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

dPDL1-4 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

dPDL1-4LYTACsPD-1/PD-L1HSPLysosome-targeting chimerasPD-1/Programmed death-ligand 1Heat shock proteinsCancereHSPTACsMC38HeLaC57BL/6J miceInhibitorinhibitorinhibit

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