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Cotransin | Inhibitor of SEC61A1
RATINGS:
Cellular Use: (3 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
SEC61A1
Inhibitor
2 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
In in vitro TNT assays, cotransin had no affect on pre-prolactin or model type I, type II, and multi ...

Potency
Cellular
In Vitro

SEC61A1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Negative Control Compounds

Nor-cotransin

Chemical Information

Molecular Formula C42H68N6O8
SMILEs CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)N(C)C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)OC(=O)[C@H](C)N(C)C1=O
InChI InChI=1S/C42H68N6O8/c1-24(2)19-31-39(52)46(11)28(9)42(55)56-29(10)36(49)43-32(20-25(3)4)40(53)47(12)34(22-27(7)8)37(50)45-33(21-26(5)6)41(54)48(13)35(38(51)44-31)23-30-17-15-14-16-18-30/h14-18,24-29,31-35H,19-23H2,1-13H3,(H,43,49)(H,44,51)(H,45,50)/t28-,29+,31-,32-,33-,34-,35-/m0/s1
Molecular weight 784.51 Da
AlogP 3.314100000000008
HBond acceptors 14
HBond donors 3
Atoms 124

References

Publications

    Cross References

    canSAR

    Expert Reviews

    by SERP
    (on 17 Jul 2017 )
    Cellular Use Rating
    Cotransin is a relatively new probe for Sec61-dependent protein translocation. This probe is the best we have so far, but there is scant information regarding precise mode of on-target action and potential...
    by SERP
    (on 14 Dec 2018 )
    Cellular Use Rating
    There has been 2015 mechanistic study “Defining a Conformational Consensus Motif in Cotransin-Sensitive Signal Sequences: PMC4373898 but the specificity does not have extensive SAR in particular for...
    by SERP
    (on 23 Nov 2020 )
    Cellular Use Rating
    Because Cotransin is signal sequence specific, it only blocks a certain subset of proteins which are translocated by SEC61. Cotransin analogues have been made which target different proteins which are...
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