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Spastazolin | Spastazolin : ATP competitive of SPAST
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
SPAST
  • IC50:99 ± 18 nM
ATP competitive
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: Spastazoline did not appreciably inhibit any of the four related ...

Potency
Cellular
In Vitro

SPAST

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-019-0225-6

Chemical Information

Molecular Formula C20H30N8
SMILEs CC(C)[C@@H]1CN(c2nc(Nc3cc(C(C)(C)C)[nH]n3)c3cc[nH]c3n2)CCN1
InChI InChI=1S/C20H30N8/c1-12(2)14-11-28(9-8-21-14)19-24-17-13(6-7-22-17)18(25-19)23-16-10-15(26-27-16)20(3,4)5/h6-7,10,12,14,21H,8-9,11H2,1-5H3,(H3,22,23,24,25,26,27)/t14-/m0/s1
Molecular weight 382.26 Da
AlogP 0.0
HBond acceptors 8
HBond donors 4
Atoms 58

Vendors

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Expert Reviews

by SERP
(on 31 May 2023 )
Cellular Use Rating
Based on the selectivity data provided, spastazoline appears to be quite selective for spastin among the 4 AAA proteins measured. That said, the off-target kinase activity against both Flt3 and NTRK1...
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