Borussertib

Borussertib : Covalent-allosteric inhibitor of AKT2, AKT1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe Borussertib is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

AKT2
AKT1

Covalent Inhibitor

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P31751

Target Class: Kinase

Target SubClass: AGC

Potency: IC50

Potency Value: 59 nM

Potency Assay: Homogeneous Time Resolved Fluorescence (HTRF) assay (AKT2)

PDB ID for probe-target interaction (3D structure): 6HHF

Target aliases:

RAC-beta serine/threonine-protein kinase, AKT2, AK ...

DOI Reference: 10.1158/0008-5472.CAN-18-2861

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family- AKT3: IC50 = 650 ± 170 nM (HTFR); IC50 = 4.3 µM (NanoBRET). SelectScreen® Kinase Profiling (100) at 1 µM: clean.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

I would not recommend dosing with this compound orally.

(last updated: 1 Mar 2022 )

Portal Comments

In a 2023 study, Hu et al. evaluated Borussertib in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI:10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)