JH-X-119-01
Based on 6 publication(s) in Google Scholar
JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM.
For research use only. We do not sell to patients.
- Purity: 99.65%
- CAS No.: 2227368-54-7
- Formula: C25H20N6O3
- Molecular Weight:452.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Publications Citing Use of MedChemExpress (MCE) JH-X-119-01
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Biological Activity
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IRAK-1 9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| OCI-LY19 | EC50 |
0.59 μM
Compound: 1; JH-X-119-01
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Cytotoxicity against human OCILY19 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human OCILY19 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 33214835] |
| OCI-Ly3 | EC50 |
9.72 μM
Compound: 1; JH-X-119-01
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Cytotoxicity against human OCILY3 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human OCILY3 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 33214835] |
| OCI-Ly7 | EC50 |
2.39 μM
Compound: 1; JH-X-119-01
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Cytotoxicity against human OCILY7 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human OCILY7 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 33214835] |
| Ramos | EC50 |
1.79 μM
Compound: 1; JH-X-119-01
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Cytotoxicity against human Ramos cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human Ramos cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 33214835] |
| RPMI-8226 | EC50 |
5.13 μM
Compound: 1; JH-X-119-01
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Cytotoxicity against human RPMI-8226 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human RPMI-8226 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 33214835] |
| TMD8 | EC50 |
2.4 μM
Compound: 1; JH-X-119-01
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Cytotoxicity against human TMD8 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human TMD8 cells expressing MYD88 mutant assessed as cell killing measured after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 33214835] |
JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation[1].? JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC50 of 57 nM for YSK4[2].? JH-X-119-01 shows moderate cell killing effects in a panel of Waldenstr?m’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC50s ranging from 0.59 to 9.72 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 cells and THP-1 cells
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Concentration:10 μM
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Incubation Time:15 minutes
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Result:Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (20-22 g, male) mice[1]
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Dosage:5 mg/kg and 10 mg/kg
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Administration:Intraperitoneally injected; 5 days
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Result:Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.
Chemical Information
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CAS No. 2227368-54-7
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Appearance Solid
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Molecular Weight 452.46
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Formula C25H20N6O3
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Color Light yellow to brown
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SMILES
O=C(C=C)NC1=CC=CC(C(NC2=CC=C(NC(C3=NC(C4=CC=NN4)=CC=C3)=O)C=C2)=O)=C1
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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
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci Adv
2024 Nov 29;10(48):eadq8122. PMID: 39602545 -
Emerg Microbes Infect
Capsid Protein Mediated Evasion of IRAK1-Dependent Signaling is Essential to Sindbis Virus Neuroinvasion and Virulence in Mice. [Abstract]2024 Dec;13(1):2300452. PMID: 38164715 -
JCI Insight
2022 Jul 8;7(13):e149825. PMID: 35801586 -
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Solvent & Solubility
DMSO : 100 mg/mL (221.01 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: ≥ 1.98 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 1.98 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.8 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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597. [Content Brief]
[2]. John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243. [Content Brief]
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 | 2.2101 mL | 11.0507 mL | 22.1014 mL | 55.2535 mL |
| 5 mM | 0.4420 mL | 2.2101 mL | 4.4203 mL | 11.0507 mL | |
| 10 mM | 0.2210 mL | 1.1051 mL | 2.2101 mL | 5.5254 mL | |
| 15 mM | 0.1473 mL | 0.7367 mL | 1.4734 mL | 3.6836 mL | |
| 20 mM | 0.1105 mL | 0.5525 mL | 1.1051 mL | 2.7627 mL | |
| 25 mM | 0.0884 mL | 0.4420 mL | 0.8841 mL | 2.2101 mL | |
| 30 mM | 0.0737 mL | 0.3684 mL | 0.7367 mL | 1.8418 mL | |
| 40 mM | 0.0553 mL | 0.2763 mL | 0.5525 mL | 1.3813 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1051 mL | |
| 60 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9209 mL | |
| 80 mM | 0.0276 mL | 0.1381 mL | 0.2763 mL | 0.6907 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5525 mL |
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