JH-X-119-01

JH-X-119-01 : Covalent inhibitor of IRAK1 and YSK4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe JH-X-119-01 is in the process of SERP review.

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Information

IRAK1

Covalent

~~up to 1 uM~~
Reviewer recommended concentration: 1-10 µM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P51617

Target Class: Kinase

Target SubClass: TKL

Potency: IC50

Potency Value: 9 nM

Potency Assay: Enzymatic assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Interleukin-1 receptor-associated kinase 1, IRAK, ...

DOI Reference: 10.1021/acsmedchemlett.0c00378

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: MAP3K19

Potency end-point : IC50 57 nM

Potency assay (off target): JH-X-119-01 showed exceptional kinome selectivity, as measured by a KINOMEScan selectivity score of S(10) = 0.01 at a concentration of 1 μM. JH-X-119-01 exhibited off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose-response analysis revealed an IC50 of 57 nM for YSK4. IC50 10000nM against IRAK4.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The IRAK1 inhibitory selectivity against IRAK4 is extremely high, so this probe should be useful for assessing sole IRAK1 activity.

(last updated: 16 Feb 2023 )

SERP Ratings

In Cell Rating

SERP Comments:

JH-X-119-01 is a well-characterized, selective modulator of IRAK1 relative to IRAK4. Cell activity depends on the line used. As such it is recommended that researchers conduct a dose-reponse as well cytoxicity profiling in parallel with appropriate controls.

(last updated: 22 Feb 2023 )