TP-061

TP-061 : Inhibitor of Brr2

Structure

SERP Rating

Probe TP-061 is in the process of SERP review.

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Information

SNRNP200

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: O75643

Target Class: Enzyme

Target SubClass: Helicase

Potency: IC50

Potency Value: 21 nM

Potency Assay: ADP-Glo ATPase assay

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

Target aliases:

U5 small nuclear ribonucleoprotein 200 kDa helicas ...

DOI Reference: 10.1016/j.bmc.2017.07.017

Uniprot ID: O75643

Target Class: Enzyme

Target SubClass: Helicase

Potency: Kd

Potency Value: 22 nM

Potency Assay: SPR

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

Target aliases:

U5 small nuclear ribonucleoprotein 200 kDa helicas ...

DOI Reference: 10.1016/j.bmc.2017.07.017

Uniprot ID: O75643

Target Class: Enzyme

Target SubClass: Helicase

Potency: IC50

Potency Value: 480 nM

Potency Assay: Helicase assay

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

Target aliases:

U5 small nuclear ribonucleoprotein 200 kDa helicas ...

DOI Reference: 10.1016/j.bmc.2017.07.017

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): TP-061 shows excellent selectivity over closely-related helicases, with no inhibition of eIF4A1, eIF4A3 and DHX29 up to 100 mM. Additional selectivity over 300 kinases using in-house assay showed none with inhibition > 50% when tested at 1 mM.

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SERP ratings and comments

No SERP comments found for TP-061