JH-X-119-01

Name: JH-X-119-01
Brand: MedChemExpress
SKU: HY-103017A
Rating: 5.0 (3 reviews)

Cat. No.: HY-103017A Purity: 99.03%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

JH-X-119-01 Chemical Structure

CAS No. : 2227368-54-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 198	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 730	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of JH-X-119-01:

JH-X-119-01 hydrochloride Get quote

3 Publications Citing Use of MCE JH-X-119-01

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View All IRAK Isoform Specific Products:

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IRAK1 IRAK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

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^[1]. 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^[2].

IC₅₀ & Target^[2]

IRAK-1

9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
OCI-LY19	EC₅₀	0.59 μM Compound: 1; JH-X-119-01	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	[PMID: 33214835]
OCI-Ly3	EC₅₀	9.72 μM Compound: 1; JH-X-119-01	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	[PMID: 33214835]
OCI-Ly7	EC₅₀	2.39 μM Compound: 1; JH-X-119-01	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	[PMID: 33214835]
Ramos	EC₅₀	1.79 μM Compound: 1; JH-X-119-01	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	[PMID: 33214835]
RPMI-8226	EC₅₀	5.13 μM Compound: 1; JH-X-119-01	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	[PMID: 33214835]
TMD8	EC₅₀	2.4 μM Compound: 1; JH-X-119-01	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	[PMID: 33214835]

In Vitro

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 Waldenström’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.

Western Blot Analysis^[1]

Cell Line:	RAW 264.7 cells and THP-1 cells
Concentration:	10 μM
Incubation Time:	15 minutes
Result:	Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65.

In Vivo

JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg^[1].

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

Animal Model:	C57BL/6 (20-22 g, male) mice^[1]
Dosage:	5 mg/kg and 10 mg/kg
Administration:	Intraperitoneally injected; 5 days
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.

Molecular Weight

452.46

Formula

C₂₅H₂₀N₆O₃

CAS No.

2227368-54-7

Appearance

Solid

Color

Light yellow to brown

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

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 : 125 mg/mL (276.27 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	2.2101 mL	11.0507 mL	22.1014 mL
5 mM	0.4420 mL	2.2101 mL	4.4203 mL
10 mM	0.2210 mL	1.1051 mL	2.2101 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

Purity: 99.03%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (249 KB) HNMR (288 KB) LCMS (96 KB)

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

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

JH-X-119-01 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:

JH-X-119-012227368-54-7IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseIRAK1MYD88Waldenstr?mmacroglobulinemiaDiffused Large B-cell LymphomaInhibitorinhibitorinhibit

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JH-X-119-01

Customer Review

Other Forms of JH-X-119-01:

JH-X-119-01 Related Antibodies

3 Publications Citing Use of MCE JH-X-119-01

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All IRAK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

JH-X-119-01 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

JH-X-119-01 Related Classifications

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