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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