covalent inhibitor of BMX



Protein target names: BMX

Mechanism of action: covalent inhibitor

In Vitro Validations

Uniprot ID: P51813
Target Class: Protein kinase
Target SubClass: TK
Potency: IC50
Potency Value: 8 nM
Potency Assay: Invitrogen SelectScreen Technology
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Cytoplasmic tyrosine-protein kinase BMX, BMX, BMX_ ...

In Cell Validations

In Vivo Data

No in Vivo Validations

Reagent authentication certificate: PDF image

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating


Based on the data in Supplementary Table 1, this probe also binds to 63 other kinases (score less than or equal to 75%) at 1 micromolar concentration. So choosing a concentration well below 1 micromolar is critical for cell based studies. In addition, this probe is equipotent against BTK. BMX-IN-1 shows better selectivity than other known inhibitors of BMX, but even this probe can bind (and perhaps inhibit) a number of other kinases at higher concentrations.

(last updated: 27 Jun 2016 )

SERP Ratings

In Cell Rating


BMX-IN-1 is an irreversible inhibitor of the kinase BMX and is the best available probe for it. It is also a potent inhibitor of BTK. In a broad kinome scan experiment (DiscoverX technology), BMX-IN-1 inhibits only 1% of the 442 kinases tested at >90% at a concentration of 1 micromolar. This is excellent selectivity. That said, there are potential off targets, so care should be taken in cell-based experiments to keep the dose as low as possible. The on-target, cell-based potency in a TEL-BMX transformed Ba/F3 cell line system is 25 nM. 1 micromolar of BMX-IN-1 inhibits autophosphorylation of BMX in RV-1 cells.

(last updated: 12 Sept 2016 )