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

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).
(Pink: Ligands for Target Protein for PROTAC and IRAK4 ligand (HY-179095); Blue: Ligands for E3 Ligase ligand (HY-A0003); Black: linker (HY-W008820)).

For research use only. We do not sell to patients.

PSP-0119

PSP-0119 Chemical Structure

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PSP-0119 Related Antibodies

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Description

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)

In Vitro

PSP-0119 (10 nM, 6 h) inhibits NF-kβ activity in THP-1 cells stably expressing NF-kβ-Luc reporter and robustly blocks IL-1β-induced activation (phosphorylation) of IRAK4 in MOLM-13 cells[1].
PSP-0119 demonstrates superior binding characteristics with the ternary complex, exhibiting a binding energy of -86.5 kcal/mol, indicating that it forms a highly stable ternary complex[1].
PSP-0119 (20 nM-5 μM, 24 h) selectively degrades IRAK4 protein in MOLM-13 cells (FLT3-mutant) (DC50 = 31.56 nM) and MV-4-11 cells (FLT3-mutant) (DC50 = 29.12 nM) without affecting THP-1 cells (FLT3-wild-type)[1].
PSP-0119 (3-40 nM, 24 h) significantly degrades IRAK1 in MV-4-11 cells, but fails to degrade IRAK1 in MOLM-13 AML cells[1].
PSP-0119 (40 nM, 24 h) results in downregulation of the ENOS-1 (alpha-enolase) gene in MOLM-13 cells[1].
PSP0119 (7 μM, 7 days) reduces CFUs formed by MV-4-11[1].
PSP-0119 (0-5 μM, 48 h) does not affect the viability of FLT-3 wt THP1 cells, but FLT-3 mutant MOLM-13 and MV-4-11 cells show reduced viability during 48 h[1].
PSP-0119 and JH-X-119-01 exhibit a significant synergistic effect on IRAK4 inhibition in MV-4-11 AML cells in vitro[1].

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

PSP-0119 Related Antibodies

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.
In Vivo

PSP-0119 (10 mg/kg, i.p., once daily, M-F) effectively inhibits the tumor growth of FLT3 mutant AML cells (MOLM-13) in mice, and no significant toxicity was observed[1].

MedChemExpress (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.
Molecular Weight

733.77

Formula

C38H39N9O7
SMILES

COC1=CC(N2CCN(CC2)C(CCCC(NC3=CC=CC4=C3CN(C4=O)C5CCC(NC5=O)=O)=O)=O)=CC=C1NC(C6=CC=CC(C7=NNC=C7)=N6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PSP-0119 Related Classifications

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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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