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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

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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