BAY1125976

Protein target name:

AKT1, AKT2

Mechanism of action:

Allosteric Inhibitor

Recommended Concentration for use in cells:

~~up to 1 uM~~

Reviewer suggested Concentration for use in cells:

up to 300 nM

Probe Availability

MedChemExpress

SelleckChem

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

Ser/Thr Protein Kinase

HUGO symbol:

HGNC:391 HGNC:392

Entrez gene ID:

207 208

Target alias:

AKT, PKB, PKB-ALPHA, PRKBA, RAC, RAC-ALPHA, HIHGHH, PKBB, PKBBETA, PRKBB, RAC-BETA

Probe Details

Chemical Probes Portal ID:

CPP2001

Probe alias:

BAY-1125976, BAY 1125976

PubChem CID:

70817911

SMILES string:

O=C(C1=NN2C(C=C1)=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)N

InChi Key:

JBGYKRAZYDNCNV-UHFFFAOYSA-N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50, KD

AKT1- 5.2/44; AKT2 - 18/36 nM Hi/Lo ATP

Potency assay:

TR‐FRET‐based in vitro kinase assays (SPR KD 2.7 (active) 1.3 (inactive) nM AKT1)

Off target activity

Potency (off target):

IC50

Off target protein and potency:

AKT3 427 nM @ 10mM ATP

Probe Selectivity in Vitro:

The selectivity of BAY 1125976 was assessed using two different kinase panels: the 230 kinase KinaseProfiler™ and the 468 kinase panel at DiscoveRx: FLT(D835Y), CKL1 and MKNK2 with 210, 310 and 330 nM, respectively

In cell validation

On target activity in cells

Potency in cells:

IC50

0.9 nM (T308)1.1 nM (S473)

Potency assay (cells):

Reduced the basal levels of AKT phosphorylation in KPL‐4 cells specific at T308 and S473, Block signalling pathway

In vivo validation

Organism:

Mice

Dose:

10 - 50 mg/Kg

Route of delivery:

Oral

Cmax:

21.1 - 28.8 ug/L

Tmax:

4.1 - 1.0 h @ 80 mg/Kg

Primary Reference

Reference (doi):

10.1002/ijc.30457 10.3390/cancers11121987

Reference (PMID):

27699769 31835495

BAY1125976

Probe Availability

Probe Information

Target Details

AKT, PKB, PKB-ALPHA, PRKBA, RAC, RAC-ALPHA, HIHGHH, PKBB, PKBBETA, PRKBB, RAC-BETA

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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BAY1125976

Probe Availability

Probe Information

Target Details

AKT, PKB, PKB-ALPHA, PRKBA, RAC, RAC-ALPHA, HIHGHH, PKBB, PKBBETA, PRKBB, RAC-BETA

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?