ALKBH5-IN-1

ALKBH5-IN-1 : Inhibitor of ALKBH5

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe ALKBH5-IN-1 is in the process of SERP review.

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Information

ALKBH5

Inhibitor

3 µM

Probe Availability:

Mcule

In Vitro Validations

Uniprot ID: Q6P6C2

Target Class: Enzyme

Target SubClass: Dioxygenase

Potency: IC50

Potency Value: 21 nM

Potency Assay: Fluorescence Polarization assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

RNA demethylase ALKBH5, OFOXD1, ABH5, ALKBH5, ALKB ...

DOI Reference: 10.1016/j.ejmech.2022.114446

Uniprot ID: Q6P6C2

Target Class: Enzyme

Target SubClass: Dioxygenase

Potency: ΔTm

Potency Value: 8.75 Celsius

Potency Assay: DSF assay with 100 µM compound

PDB ID for probe-target interaction (3D structure): --

Target aliases:

RNA demethylase ALKBH5, OFOXD1, ABH5, ALKBH5, ALKB ...

DOI Reference: 10.1016/j.ejmech.2022.114446

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): The selectivity of 20m against other AlkB subfamily members was assessed by DSF assay and FP assay. In the DSF assay 100 μM 20m only stabilized ALKBH5 with the ΔTm value higher than 2 °C. In the FP assay, 20m could only disrupt ALKBH5 binding to m6A substrate, whereas it failed to compete on FTO or ALKBH1 binding to m6A substrate (IC50 > 25 μM).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

From the data provided in Fang et al 2022, Fig 5A, CETSA activity at was measured at 100uM only and the fact that Fig 5B that was not quantitative, its very difficult to define cellular active concentration.

(last updated: 29 Oct 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

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 evaluation. Its selectivity against three other AlkB subfamily members was shown. However, further quantitative in-cell validation and a broader selectivity screening would be needed.

(last updated: 17 Jun 2024 )