JH-IX-179

JH-IX-179 : Inhibitor of FLT3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe JH-IX-179 is in the process of SERP review.

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Information

FLT3 (Mutant:FLT3-ITD, FLT3-N841I, and FLT3-D835V)

Inhibitor

up to 100 nM

Probe Availability:

MCULE

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

KinomeScan binding analysis against a near-comprehensive panel of 456 kinases at a concentration of 1 μM. JH-IX-179 resulted in no interactions other than FLT3 and FLT3 mutants with greater than 95% inhibition, with the exception of CIT, ROCK2, PHKG1, and CLK1. ROCK2 kinase activity IC50 936 nM, PHKG1 IC50 78 nM, and CLK4 IC50 142 nM

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a potent FLT3 inhibitor. For some off-targets, especially CIT and FLT3-wt as well as other FLT-3 mutations, no IC50 values were determined, even though the compound showed significant inhibition for them in the broad DiscoverX Kinase Panel. In particular, IC50 for FLT3-wt would be desirable. Otherwise the compound shows good activity and selectivity, especially against other prominent off-targets of FLT3 inhibitors and is the most selective inhibitor available for the FLT-ITD and FLT-D835V mutations

(last updated: 17 Jun 2024 )