STK16-IN-1

STK16-IN-1 : ATP competitive inhibitor of STK16

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe STK16-IN-1 is in the process of SERP review.

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Information

STK16

ATP competitive

up to 10 uM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: O75716

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 295 nM

Potency Assay: Invitrogen SelectScreen Biochemical assay

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

Target aliases:

Serine/threonine-protein kinase 16, TSF1, PKL12, M ...

DOI Reference: 10.1021/acschembio.6b00250

Uniprot ID: O75716

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 910 nM

Potency Assay: IP kinase assay monitoring phosphorylation of T37/46 of 4EBP1

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

Target aliases:

Serine/threonine-protein kinase 16, TSF1, PKL12, M ...

DOI Reference: 10.1021/acschembio.6b00250

Uniprot ID: O75716

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 1200 nM

Potency Assay: IP kinase assay of STK16-IN-1 with DRG1 as a substrate (detection of the general threonine phosphorylation).

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

Target aliases:

Serine/threonine-protein kinase 16, TSF1, PKL12, M ...

DOI Reference: 10.1021/acschembio.6b00250

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity profiling using DiscoveRx’s KinomeScan technology proved that among the 442 kinases tested, STK16-IN-1 only potently inhibited STK16 (relative activity remaining 0.65%) and mTOR (relative activity remaining 0.4%) at a concentration of 10 μM. Further enzymatic assays indicated mTOR IC50 >5 uM. STK16-IN-1 inhibited PI3Kδ with an IC50 of 0.856 μM, PI3Kγ with an IC50 of 0.867 μM, and other isoforms with an IC50 greater than 1 μM.

Potency assay, off target (cells): STK16-IN-1 did not exhibit any apparent inhibitory activity against four class I isoforms of PI3K up to 10 μM.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

In an in vitro potency characterisation, STK16-IN-1 demonstrated an IC50 value of 295 nM in enzymatic assay (LifeTechnology SelectScreen). Selectivity was tested by DiscoverRx KinomeScan against 442 kinases, showing high selectivity for STK16 alongside with activity against mTOR at 10 µM. Sufficient proof for cellular target engagement by STK16-IN-1 hasn't been shown. No control compounds were tested.

(last updated: 17 Jun 2024 )