2. PROTAC Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. PROTACs RIP kinase Apoptosis Caspase PARP
  4. LD5097

LD5097 是一种高效且选择性的 PROTAC 降解剂，靶向 RIPK1。LD5097 可快速有效地下调 RIPK1，并显著增强 Jurkat 细胞中 TNFα 介导的细胞凋亡 (apoptosis)。LD5097 可显著提高裂解型 caspase-3/7 和 PARP 的水平。LD5097 可用于急性 T 淋巴细胞白血病的研究。
(粉色: RIPK1 配体 (HY-179235)；蓝色: VHL 配体 (HY-47070)；黑色: 连接子 (HY-179236))。

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LD5097

LD5097 Chemical Structure

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     可免费申领三个不同产品的试用装。

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Customer Review

LD5097 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 RIP kinase 亚型特异性产品:

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RIPK1 RIPK2 RIPK3

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LD5097 is a highly effective and selective PROTAC degrader targeting RIPK1. LD5097 can rapidly and efficiently downregulate RIPK1 and significantly enhance TNFα-mediated apoptosis in Jurkat cells. LD5097 significantly increases the levels of cleaved caspase-3/7 and PARP. LD5097 can be used for the study of acute T-lymphoblastic leukemia[1]. (Pink: RIPK1 ligand (HY-179235); Blue: VHL ligand (HY-47070); Black: linker (HY-179236)).

IC50 & Target[1]

Caspase-3

 

Caspase-7

 

体外研究
(In Vitro)

LD5097 (Compound 24b) (24 小时) 在 Jurkat nLuc-RIPK1 细胞中表现出强效的 RIPK1 降解活性 (DC50 = 0.7 nM)[1]。
LD5097 (1.6-1000 nM，24 小时) 在 Jurkat 细胞中导致内源性 RIPK1 剂量依赖性降解(DC50 = 2.6 nM)[1]。
LD5097 对内源性 RIPK1 具有强效降解作用，在 MOLM14 和 U937 细胞中的 DC50 值分别为 2.8 nM 和 0.8 nM[1]。
LD5097 (100 nM，0.5-24 小时) 可在 2 小时内完全降解 Jurkat 细胞中的 RIPK1[1]。
LD5097 (100 nM，24 小时) 的降解能力依赖于双功能 PROTAC 机制，该机制需要同时结合 RIPK1 和 VHL E3 连接酶[1]。
LD5097 (100 nM，72 小时) 可增强 Jurkat 细胞中 TNFα 介导的细胞凋亡[1]。
LD5097 (0-10 μM，24 小时) 在 Ramos 细胞中浓度为 100 nM 时可完全降解 RIPK1，但在 A20 细胞中即使浓度为 10 μM 也无法完全降解 RIPK1[1]。

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

LD5097 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 100 nM
Incubation Time: 0.5 h, 1 h, 2 h, 4 h, 6 h, 12 h, 24 h
Result: Completely degraded RIPK1 in Jurkat cells within 2 hours.

Apoptosis Analysis[1]

Cell Line: Jurkat cells
Concentration: 100 nM
Incubation Time: 72 h
Result: Combined with TNFα significantly induced apoptosis.
Cleaved caspase-3/7 and PARP levels increased.
Apoptosis could be reversed by Z-VAD-FMK (HY-16658B).

Western Blot Analysis[1]

Cell Line: Ramos cells, A20 cells
Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Complete degradation of RIPK1 at 100 nM in Ramos cells, but failed to do so even at 10 μM in A20 cells.
体内研究
(In Vivo)

LD5097 (Compound 24b) (10 mg/kg，静脉注射，一次) 可显著降解 Jurkat 细胞异种移植小鼠肿瘤中的 RIPK1[1]。

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

Animal Model: 6-week-old female nude mice were subcutaneously injected with 2.5 × 106 Jurkat cells suspended in a 1:1 mixture with Matrigel[1].
Dosage: 10 mg/kg
Administration: I.v., once
Result: Induced a decrease of more than 70% in RIPK1 protein levels in tumor tissue at both 6 and 24 hours after administration.
分子量

1382.53

Formula

C74H75F4N13O8S
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

LD5097 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 *
= × ×

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:

LD5097LD 5097LD-5097PROTACsRIP kinaseApoptosisCaspasePARPReceptor-interacting protein kinasesRIPKpoly ADP ribose polymeraseRIPK1 DegradersPROTACJurkat Xenograft ModelInhibitorinhibitorinhibit

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目录号：
HY-179234
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