2. PROTAC Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. PROTACs IRAK NF-κB Enolase
  4. PSP-0119

PSP-0119 是一种高效的 PROTAC 降解剂，靶向 IRAK4 (IC50 = 2.83 nM) 。PSP-0119 可抑制 IRAK4 激酶活性、NF-κβ 活性以及 IL-1β 诱导的 IRAK4 磷酸化。PSP-0119 可降解 FLT3 突变型 AML 细胞系中的 IRAK4，但不影响 FLT3 野生型 AML 细胞、FLT3 野生型样本和正常骨髓。PSP-0119 可下调 MOLM-13 细胞中的 alpha-enolase (eNOS) 表达。PSP-0119 可用于急性髓系白血病 (AML) 的研究。
(粉色: Ligands for Target Protein for PROTAC 和 IRAK4 配体 (HY-179095)；蓝色: Ligands for E3 Ligase 配体 (HY-A0003)；黑色: 连接子 (HY-W008820))。

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PSP-0119

PSP-0119 Chemical Structure

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Customer Review

PSP-0119 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 IRAK 亚型特异性产品:

查看所有亚型
IRAK1 IRAK4

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML)[1]. (Pink: Ligands for Target Protein for PROTAC and IRAK4 ligand (HY-179095); Blue: Ligands for E3 Ligase ligand (HY-A0003); Black: linker (HY-W008820)).

IC50 & Target

NF-κB

 

IRAK4

2.83 nM (IC50)

体外研究
(In Vitro)

PSP-0119 (10 nM，6 小时) 可抑制稳定表达 NF-κB-Luc 报告基因的 THP-1 细胞中的 NF-κB 活性，并能显著阻断 IL-1β 诱导的 MOLM-13 细胞中 IRAK4 磷酸化[1]。
PSP-0119 与三元复合物具有优异的结合特性，其结合能为 -86.5 kcal/mol，表明其能形成高度稳定的三元复合物[1]。
PSP-0119 (20 nM-5 μM，24 小时) 可选择性地降解 MOLM-13 细胞 (FLT3 突变型) (DC50 = 31.56 nM) 和 MV-4-11 细胞 (FLT3 突变型) (DC50 = 29.12 nM) 中的 IRAK4 蛋白，而对 THP-1 细胞 (FLT3 野生型) 无影响[1]。
PSP-0119 (3-40 nM，24 小时) 可显著降解 MV-4-11 细胞中的 IRAK1，但不能降解 MOLM-13 AML 细胞中的 IRAK1[1]。
PSP-0119 (40 nM，24 小时) 可下调 MOLM-13 细胞中 ENOS-1 (α-烯醇化酶) 基因的表达[1]。
PSP-0119 (7 μM，7 天) 可减少 MV-4-11 细胞形成的菌落形成单位 (CFU)[1]。
PSP-0119 (0-5 μM，48 小时) 不影响 FLT-3 野生型 THP1 细胞的活力，但 FLT-3 突变型 MOLM-13 和 MV-4-11 细胞在 48 小时内活力降低[1]。
PSP-0119 和 JH-X-119-01 在体外对 MV-4-11 AML 细胞中的 IRAK4 抑制表现出显著的协同作用[1]。

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

PSP-0119 相关抗体:

Western Blot Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 10 nM
Incubation Time: 6 h
Result: Blocked IL-1β induced activation (phosphorylation) of IRAK4 in MOLM-13 cells.

Western Blot Analysis[1]

Cell Line: THP-1 cells (FLT3-wild-type) , MOLM-13 cells (FLT3-mutant) , MV-4-11 cells (FLT3-mutant)
Concentration: 3 nM, 7 nM, 20 nM, 40 nM, 1.25 µM, 2.5 µM, 5 µM
Incubation Time: 24 h
Result: Did not downregulate IRAK4 expression in THP1 cells until the tested doses of 5 µM.
IRAK4 expression in FLT3-mutant MV-4-11 and MOLM-13 cells was reduced between doses 20-40 nM doses.

Cell Viability Assay[1]

Cell Line: THP-1 cells (FLT3-wild-type) , MOLM-13 cells (FLT3-mutant) , MV-4-11 cells (FLT3-mutant)
Concentration: 0μM, 2.5μM, 5μM
Incubation Time: 48 h
Result: Did not affect the viability of FLT-3 wt THP1 cells, but FLT-3 mutant MOLM-13 and MV-4-11 cells showed reduced viability during 48 h.
体内研究
(In Vivo)

PSP-0119 (10 mg/kg，腹腔注射，每日一次，周一至周五) 能有效抑制小鼠体内 FLT3 突变 AML 细胞 (MOLM-13) 的肿瘤生长，且未观察到明显的毒性[1]。

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

Animal Model: Viable MOLM-13 cells (3 million cells/mice) were suspended in cold Matrigel: RPMI media (without serum and antibiotics) (1:1) and injected into the right flank of female NSG mice (100 μL/mice)[1].
Dosage: 10 mg/kg
Administration: I.p., once daily, Monday to Friday
Result: Significantly inhibited tumor growth.
分子量

733.77

Formula

C38H39N9O7
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

PSP-0119 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:

PSP-0119PSP0119PSP 0119PROTACsIRAKNF-κBEnolaseInterleukin-1 receptor associated kinaseIL-1R associated kinaseNuclear factor-κBNuclear factor-kappaBPhosphopyruvate hydrataseIRAK4PROTACAcute Myeloid LeukemiaAMLFLT3-mutant AMLInhibitorinhibitorinhibit

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