MU1210

MU1210 : Inhibitor of CLK1, CLK2, CLK4

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

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Information

CLK1
CLK2
CLK4

Inhibitor

up to 1 uM
Reviewer recommended concentration: 500 nM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P49759

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 8 nM

Potency Assay: Biochemical assay

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

Target aliases:

Dual specificity protein kinase CLK1, CLK, CLK1, C ...

DOI Reference: 10.1016/j.ejmech.2021.113299

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): MU1210 is selective in a panel of 210 kinases in an activity-based assay (Invitrogen) at 1 µM. The closest off-target is HIPK2 (IC50 of 23 nM; >5x).

Potency assay, off target (cells): HIPK2 and GSK3A/B activity was analysed via NanoBRET in cells and reported not active at 10uM against these targets. In NanoBRET assay, MU1210 also shows a potency of 1.7 µM against the splicing kinase DYRK2.

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 19 May 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Chemical probe for CLK1, CLK2, CLK4 with nanomolar potency in biochemical (radiometric assay) and cell-based (NanoBRET) assays. Kinase selectivity was tested in a panel of 210 kinases. HIPK2 (activity-based assay, radiometric assay) seems to be a potential off-target but does not show binding in the cellular NanoBRET assays (up to 10µM). However, a mono-selective probe would be appreciated. Negative control (MU140) with no activity up to 10 µM (NanoBRET) is commercially available.

(last updated: 17 Jun 2024 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This compound shows good in vitro potency of 8/20/12 nM for CLK1/2/4, respectively. Also it has good cellular potency of 84/91/23 nM for CLK1/2/4, respectively. It was screened for 210 kinases in an activity-based assay and the only off-target was HIPK2 which shows 5x weaker IC50 value than CLK family but in NanoBRET this compound didn't inhibit HIPK2. A negative control MU140 has been characterised in vitro and in vivo assays. MU1210 was not toxic in cells at >1uM after 24 hours so I would evaluate this compound as promising compound in vitro and in cells.

(last updated: 23 Sept 2024 )