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Bistramide A | Bistramide A : Disruptor of ACTG2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ACTG2
  • KD:7 nM
  • GI50:20.4 nM
Actin disruptor
50-100 nM

Selectivity

Potency
Cellular
In Vitro

ACTG2

Mode of Action: Actin disruptor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/np50112a002

Chemical Information

Molecular Formula C40H68N2O8
SMILEs C/C=C/C(=O)C[C@H]1CC[C@H](C)[C@H](CC(=O)NC[C@H](O)[C@H](C)C(=O)NCCC[C@H]2O[C@@]3(CCC[C@H](CC[C@H](C)/C=C(\C)[C@H](C)O)O3)CC[C@@H]2C)O1
InChI InChI=1S/C40H68N2O8/c1-8-11-32(44)23-34-17-15-27(3)37(48-34)24-38(46)42-25-35(45)30(6)39(47)41-21-10-13-36-28(4)18-20-40(50-36)19-9-12-33(49-40)16-14-26(2)22-29(5)31(7)43/h8,11,22,26-28,30-31,33-37,43,45H,9-10,12-21,23-25H2,1-7H3,(H,41,47)(H,42,46)/b11-8+,29-22+/t26-,27-,28-,30-,31-,33+,34+,35-,36+,37-,40-/m0/s1
Molecular weight 704.50 Da
AlogP 5.929
HBond acceptors 10
HBond donors 4
Atoms 118

References

Publications

Cross References

canSARChEMBL

Expert Reviews

by SERP
(on 17 Jul 2017 )
Cellular Use Rating
Portal staff comment: Bistramide A is not a PKC δ activator.
by SERP
(on 24 Jul 2017 )
Cellular Use Rating
In Model Organisms
Bistramide A is a novel actin-binding compound that disrupts actin filament formation. The compound has a fairly narrow concentration range and can be used as an orthogonal probe to study actin dynamics. ...
by SERP
(on 16 Nov 2020 )
Cellular Use Rating
Bistramide A, at submicromolar concentrations, is shown to bind G-actin and sequester the actin molecule from polymerization into F-actin in cells, but at concentrations higher that 10 uM, the compound...
Bistramide A displays good affinity for actin with Kd=7nM. Its activity in cells is reported in the range of 20mM to 750nM (PMID 3238698 and 7807120) depending on the readout and cancer cell line tested....
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