BMX-IN-1

BMX-IN-1 : covalent inhibitor of BMX

Structure

Information

  • BMX
  • covalent inhibitor
  • Up to 25 nM

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

Off-Target Selectivity Assesments

Potency end-point : IC50 BTK 10.4 nM
Potency assay (off target): Assessed activity against 442 kinases using the KinomeScan approach
Potency in cells, off target : GI50 TEL-JAK1 4.92 uM, TEL-JAK2 5.83 uM, TEL-JAK3 7.98 uM, TEL-TYK2 E957D 6.09 uM, TEL-BLK 3.64 uM
Potency assay, off target (cells): Inhibits the proliferation of a panel of murine Ba/F3 cells that were transformed with TEL fusion of BMX.
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SERP ratings and comments


SERP Ratings

In Cell Rating

SERP Comments:

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

(last updated: 6 Jul 2016 )

SERP Ratings

In Cell Rating

SERP Comments:

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 )