ALKBH5-IN-1 | ALKBH5-IN-1 : Inhibitor of ALKBH5
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
In Vivo

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ALKBH5
  • IC50:21 nM
  • ΔTm:8.75 Celsius
  • ΔTm:~10 Celsius
Inhibitor
3 µM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
The selectivity of 20m against other AlkB subfamily members was assessed by DSF assay and FP assay. ...

Potency
Cellular
In Vitro

ALKBH5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ejmech.2022.114446

Negative Control Compounds

cpd 20n
Notes: cpd 20n has an IC50 ~5000 nM in FP assay
ChEMBL ID: CHEMBL5207507

Chemical Information

Molecular Formula C11H7F3N2O3
SMILEs O=C(O)c1cc(O)n(-c2cccc(C(F)(F)F)c2)n1
InChI InChI=1S/C11H7F3N2O3/c12-11(13,14)6-2-1-3-7(4-6)16-9(17)5-8(15-16)10(18)19/h1-5,17H,(H,18,19)
Molecular weight 272.04 Da
AlogP 0.0
HBond acceptors 5
HBond donors 2
Atoms 26

Vendors

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Expert Reviews


(on 29 Oct 2023)
Cellular Use Rating
...
(on 17 Jun 2024)
Cellular Use Rating
Compound 20m is an inhibitor of ALKBH5. It binds with good potency as verified by DSF and FP assay. In-cell activity was only determined by CETSA @ 100µM and by demethylation assay without quantitative...
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