BSJ-04-122

BSJ-04-122 : Covalent of MAP2K4, MAP2K7

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe BSJ-04-122 is in the process of SERP review.

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Information

MAP2K4
MAP2K7

Covalent

up to 10 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P45985

Target Class: Kinase

Target SubClass: STE

Potency: IC50

Potency Value: 4 nM

Potency Assay: Lanthascreen binding assay; covalent binding to CYS247, located before the highly conserved DFG motif, was confirmed by LC-MS

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

Target aliases:

Dual specificity mitogen-activated protein kinase ...

DOI Reference: 10.1016/j.chembiol.2020.08.014

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): MKK4 and MKK7 are the top targets bound by BSJ-04-122 in MDA-MB-231 cells pretreated with the compound for 6 h (with 90.2% and 87.0%, respectively), whereas most protein kinases were not affected.

Potency assay (off target): BSJ-04-122 was profiled against a broader kinase panel using the KINOMEscan approach: a total of 26 kinases, including MKK4 and MKK7, were detected with more than 80% inhibition at 1 μM compared with DMSO control. Other than MKK family other kinases don't have the catalytic cysteine.

Potency assay, off target (cells): Selectivity within target family: BSJ-04-122 had no effect on the phosphorylation of p38, a downstream effector of MKK3/6. Similarly, the MKK1/2 and MKK5 pathways were also not inhibited, as assessed by phosphorylation levels of downstream substrates ERK1/2 and ERK5

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

There may be cross-reactivity with other kinases at 10uM, as quite a few kinases are nearly completely inhibited by this compound at 1uM (in biochemical assays). Thus, it would be wise to perform experiments at multiple concentrations, with 10uM as the absolute maximum.

(last updated: 4 Jan 2023 )

SERP+ Ratings

In Cell Rating

(last updated: 22 Mar 2023 )