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AC-4-130 | AC-4-130 : Inhibitor of STAT5B
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
STAT5B
  • IC50:1700 nM
Inhibitor
up to 2 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
RNA-seq using FLT3-ITD+ cell lines MV4–11 and MOLM-13 after inhibitor treatment 5 uM
Selectivity Assessment Description:
Downregulation of 1418 genes and upregulation of 752 genes in both cell lines was observed.

Potency
Cellular
In Vitro

STAT5B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41375-017-0005-9

In Vivo Validations

Mouse
Dose: 25 mg/Kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1038/s41375-017-0005-9

Orthogonal Probes def

Pimozide
PICEATANNOL

Chemical Information

Molecular Formula C37H36ClF5N2O5S
SMILEs CC(C)(C)c1cc(CN(C(=O)CN(Cc2ccc(Cl)cc2)S(=O)(=O)c2c(F)c(F)c(F)c(F)c2F)c2ccc(C(=O)O)cc2)cc(C(C)(C)C)c1
InChI InChI=1S/C37H36ClF5N2O5S/c1-36(2,3)24-15-22(16-25(17-24)37(4,5)6)19-45(27-13-9-23(10-14-27)35(47)48)28(46)20-44(18-21-7-11-26(38)12-8-21)51(49,50)34-32(42)30(40)29(39)31(41)33(34)43/h7-17H,18-20H2,1-6H3,(H,47,48)
Molecular weight 750.20 Da
AlogP 8.753000000000002
HBond acceptors 7
HBond donors 1
Atoms 87

Vendors

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Expert Reviews

by SERP
(on 26 Jul 2020)
Cellular Use Rating
In Model Organisms
This compound is potent and has nice selectivity for STAT5B over STAT3, but there is no analysis in the literature of other targets of this molecule, so it should be used with some caution. As for in...
by SERP
(on 28 Aug 2020)
Cellular Use Rating
In Model Organisms
In the “Leukemia” key publication (doi: 10.1038/s41375-017-0005-9) the authors present the STAT5 inhibitor AC-4-130 as a new therapeutic agent for haematological malignancies. They showed an effect...
by SERP
(on 12 Oct 2020)
Cellular Use Rating
In Model Organisms
The probe represents one of the first STAT5 inhibitors targeting the SH2 domain. However, while cellular data are convincing, current literature does not characterise the probe well in vitro using binding...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria