PSP-0119
Based on 1 Customer Validation
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.
- Purity: 98.65%
- CAS No.: 3104855-98-0
- Formula: C38H39N9O7
- Molecular Weight:733.77
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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NF-κB |
IRAK4 2.83 nM (IC50) |
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.
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Cell Line:MOLM-13 cells
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Concentration:10 nM
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Incubation Time:6 h
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Result:Blocked IL-1β induced activation (phosphorylation) of IRAK4 in MOLM-13 cells.
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Cell Line:THP-1 cells (FLT3-wild-type) , MOLM-13 cells (FLT3-mutant) , MV-4-11 cells (FLT3-mutant)
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Concentration:3 nM, 7 nM, 20 nM, 40 nM, 1.25 µM, 2.5 µM, 5 µM
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Incubation Time:24 h
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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.
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Cell Line:THP-1 cells (FLT3-wild-type) , MOLM-13 cells (FLT3-mutant) , MV-4-11 cells (FLT3-mutant)
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Concentration:0μM, 2.5μM, 5μM
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Incubation Time:48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:10 mg/kg
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Administration:I.p., once daily, Monday to Friday
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Result:Significantly inhibited tumor growth.
Chemical Information
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CAS No. 3104855-98-0
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Appearance Solid
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Molecular Weight 733.77
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Formula C38H39N9O7
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Color Light yellow to green yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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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