MSC1186

MSC1186 : Inhibitor of SRPK1, SRPK2, SRPK3

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe MSC1186 is in the process of SERP review.

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Information

SRPK1
SRPK2
SRPK3

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q96SB4

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 2.7 nM

Potency Assay: Biochemical activity assay performed at Reaction Biology

PDB ID for probe-target interaction (3D structure): 7PQS

Target aliases:

SRSF protein kinase 1, SRPK1, SRPK1_HUMAN, SR-prot ...

DOI Reference: 10.1021/acs.jmedchem.2c01705

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

MSC2711186 was selective in an in vitro kinase panel from Reaction Biology at 1 µM against 395 Kinases, followed by cellular NanoBRET assays.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Only one off-target, MAPK14, has been determined. Structure alert: the compound is a potential metal chelator for e.g., Zn, Cu, Mn, and Fe ions. It has insufficient solubility for animal studies. There are some discrepancies between Figure 9 and Table 5 for cell lysates.

(last updated: 22 Mar 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

In terms of selectivity SRPK1, SRPK2 and SRPK3 should be regarded as isoforms, and hence, the inhibitor is expected to be active on all three. Selectivity within family (kinases) has been evaluated well in biochemical assay demonstrating no off-target activity.

(last updated: 23 May 2024 )