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MSC1186 | MSC1186 : Inhibitor of SRPK1, SRPK2, SRPK3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SRPK1
  • IC50:2.7 nM
  • IC50:98 nM
  • IC50:44 nM
SRPK2
  • IC50:81 nM
  • Kd:145 nM
  • IC50:149 nM
SRPK3
  • IC50:0.59 nM
  • IC50:40 nM
  • IC50:20 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
MSC2711186 was selective in an in vitro kinase panel from Reaction Biology at 1 µM against 395 Kinas ...

Potency
Cellular
In Vitro

SRPK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c01705

SRPK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c01705

SRPK3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c01705

Negative Control Compounds

CANSAR3550540
Notes: MSC5360 shows no activity in biochemical assays and no activity was detected by NanoBRET assays in intact and in lysed cells

Chemical Information

Molecular Formula C19H17ClFN7O2S
SMILEs CN(c1ncccc1CNc1ccnc(-c2nc3c(F)c(Cl)ccc3[nH]2)n1)S(C)(=O)=O
InChI InChI=1S/C19H17ClFN7O2S/c1-28(31(2,29)30)19-11(4-3-8-23-19)10-24-14-7-9-22-17(26-14)18-25-13-6-5-12(20)15(21)16(13)27-18/h3-9H,10H2,1-2H3,(H,25,27)(H,22,24,26)
Molecular weight 461.08 Da
AlogP 0.0
HBond acceptors 9
HBond donors 2
Atoms 48

Expert Reviews

by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
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...
by SERP+
(on 23 May 2024 )
Cellular Use Rating
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...
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