AB680

AB680 : Reversible Competitive Inhibitor of NT5E

Structure

Information

Protein target names: NT5E

Mechanism of action: Reversible Competitive Inhibitor

Recommended in-cell concentration:
200 nM

Reviewer recommended in-cell concentration: 0.4–4 nM

Primary References:

In Vitro Validations

Uniprot ID: P21589
Target Class: Other
Target SubClass: Membrane Protein
Potency: Ki, IC50
Potency Value: 5 pM, 43 pM
Potency Assay: AMP-Glo assay, Enzymatic reaction
PDB ID for probe-target interaction (3D structure): 6Z9D
Structure-activity relationship: yes
Target aliases:
5'-nucleotidase, NTE, NT5, NT5E, 5NTD_HUMAN, 5'-NT ...

In Cell Validations

In Vivo Data

I have extra information to add

SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 10 Aug 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 10 Aug 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

High levels of adenosine with the tumor microenvironment inhibit the activation of T cells and NK cells thereby suppressing the immune function. CD73 is ecto-nucleotidase which catalyses the conversion of adenosine monophosphate (AMP) to adenosine.  AB680 is a highly selective inhibitor of the ecto-nucleotidase CD73 however it is a triply charged molecule that requires iv delivery.  AB680 demonstrates excellent potency (Ki =5 pM). Furthermore, it shows a desirable slow clearance in several animal models including mouse, rat, dog, and monkey.

(last updated: 5 Sept 2020 )