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: IRAK4 ligand (HY-179095); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W008820)).

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

PSP-0119

PSP-0119 Chemical Structure

CAS No. : 3104855-98-0

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Customer Review

Based on 1 publication(s) in Google Scholar

PSP-0119 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All IRAK Isoform Specific Products:

View All Isoforms
IRAK1 IRAK3 IRAK4

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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: IRAK4 ligand (HY-179095); Blue: Cereblon 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
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (136.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3628 mL 6.8141 mL 13.6282 mL
5 mM 0.2726 mL 1.3628 mL 2.7256 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3628 mL 6.8141 mL 13.6282 mL 34.0706 mL
5 mM 0.2726 mL 1.3628 mL 2.7256 mL 6.8141 mL
10 mM 0.1363 mL 0.6814 mL 1.3628 mL 3.4071 mL
15 mM 0.0909 mL 0.4543 mL 0.9085 mL 2.2714 mL
20 mM 0.0681 mL 0.3407 mL 0.6814 mL 1.7035 mL
25 mM 0.0545 mL 0.2726 mL 0.5451 mL 1.3628 mL
30 mM 0.0454 mL 0.2271 mL 0.4543 mL 1.1357 mL
40 mM 0.0341 mL 0.1704 mL 0.3407 mL 0.8518 mL
50 mM 0.0273 mL 0.1363 mL 0.2726 mL 0.6814 mL
60 mM 0.0227 mL 0.1136 mL 0.2271 mL 0.5678 mL
80 mM 0.0170 mL 0.0852 mL 0.1704 mL 0.4259 mL
100 mM 0.0136 mL 0.0681 mL 0.1363 mL 0.3407 mL
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PSP-0119 Related Classifications

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-01193104855-98-0PSP0119PSP 0119PROTACsIRAKNF-κBEnolaseInterleukin-1 receptor associated kinaseIL-1R associated kinaseNuclear factor-κBNuclear factor-kappaBPhosphopyruvate hydrataseIRAK4PROTACAcute Myeloid LeukemiaAMLFLT3-mutant AMLInhibitorinhibitorinhibit

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