2. PROTAC Immunology/Inflammation Apoptosis
  3. PROTACs IRAK Interleukin Related TNF Receptor
  4. LZ-07

LZ-07 是一种 IRAK4 PROTAC 降解剂 (DC50 = 1.14 nM)。降解 IRAK4 后，LZ-07 可显著抑制 IL-6、IL-1β、TNF-α 和 IL-10 等细胞因子的表达。LZ-07 可用于自身免疫性疾病的研究 (粉色：IRAK4 配体 (HY-172591)；蓝色：CRBN 配体 (HY-W883357)；黑色：连接子 (HY-B0149)；CRBN 配体 + 连接子：HY-172593)。

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LZ-07 Chemical Structure

LZ-07 Chemical Structure

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LZ-07 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 IRAK 亚型特异性产品:

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IRAK1 IRAK4

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593)[1].

体外研究
(In Vitro)

LZ-07 (10-100 nM，16 小时) 在 THP-1 细胞系中表现出最强的降解活性，在 10 nM 时降解水平超过 65%，在 100 nM 时降解水平超过 75%[1]。
LZ-07 (0.3-300 nM，16 小时) 在 DOHH2 和 TMD8 细胞中表现出剂量依赖性的 IRAK4 降解(DC50 分别为 1.14 nM 和 2.70 nM)[1]。
LZ-07 (0.3-300 nM，0-24 小时) 在 50 nM 浓度下 4 小时内诱导快速显著的降解，在 TMD8 细胞中 16 小时时达到最大降解 (Dmax = 91%)，并在 DOHH2 细胞中降解 IRAK4迅速[1]。
LZ-07 (30 nM，8小时) 通过泛素-蛋白酶体系统介导 IRAK4 降解，其活性依赖于与 IRAK 和CRBN 的结合[1]。
LZ-07 (3.9-7.6 nM，2小时) 在 LPS (100 ng/mL) 刺激的 PBMC 中表现出对四种关键炎症细胞因子 (IL-6、IL-10、IL-1β和TNF-α) 的优异抑制作用[1]。

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

LZ-07 相关抗体:

Western Blot Analysis[1]

Cell Line: Pretreated DOHH2 and TMD8 cells with DMSO, MG132 (HY-13259) (0.5 μM), MLN4924 (HY-70062) (0.5 μM), Pomalidomide (HY-10984) (1 μM) and Compound E (1 μM)
Concentration: 30 nM
Incubation Time: 8 h
Result: Inhibited IRAK4 degradation and the degradation was blocked by pretreatment of proteasome inhibitor MG132, the ubiquitination inhibitor MLN4924, compound E and pomalidomide.

ELISA Assay[1]

Cell Line: LZ-07 pretreated PBMCs with LPS stimulation (100 ng/mL)
Concentration: 3.9-7.6 nM
Incubation Time: 2 h pretreatment, followed by stimulation with LPS for 24 h
Result: Exhibited 131-fold greater inhibition of IL-6 compared to KT-474 (HY-145483) in PBMCs from one healthy donor.
Inhibited IL-6 with an IC50 of 4.8 nM in PBMC from another donor.
Inhibited key inflammatory cytokines including IL-6, IL-10, IL-1β and TNF-α.
分子量

812.92

Formula

C42H48N14O4
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

LZ-07 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

LZ-07LZ07LZ 07PROTACsIRAKInterleukin RelatedTNF ReceptorInterleukin-1 receptor associated kinaseIL-1R associated kinaseILTumor Necrosis Factor ReceptorTNFRDegraderautoimmunecytokinesInhibitorinhibitorinhibit

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目录号：
HY-172590
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