RBN-2397

RBN-2397 : NAD+ competitive of PARP7

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe RBN-2397 is in the process of SERP review.

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Information

TIPARP

NAD+ competitive

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q7Z3E1

Target Class: Other post-translational modification

Target SubClass: PARP

Potency: IC50

Potency Value: <3 nM

Potency Assay: Probe displacement assay

PDB ID for probe-target interaction (3D structure): 6V3W

Target aliases:

Protein mono-ADP-ribosyltransferase TIPARP, PARP7, ...

DOI Reference: 10.1016/j.ccell.2021.06.018

Uniprot ID: Q7Z3E1

Target Class: Other post-translational modification

Target SubClass: PARP

Potency: Kd

Potency Value: 0.22 nM

Potency Assay: SPR (ka = 1.65 × 105 (1/Ms), kd = 3.56 × 10-5 (1/s) and t1/2 = 325 min)

PDB ID for probe-target interaction (3D structure): 6V3W

Target aliases:

Protein mono-ADP-ribosyltransferase TIPARP, PARP7, ...

DOI Reference: 10.1016/j.ccell.2021.06.018

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: >50-fold selectivity for inhibition of PARP7 over all PARP family members Selectivity outside target family: Activity of RBN-2397 in a panel of 58 kinases and 44 safety-related targets including GPCRs, ion channels, nuclear receptors, and selected enzymes.

Potency assay, off target (cells): RBN-2397 inhibits MARylation of multiple intracellular proteins in PARP7-overexpressing SK-MES-1 cells with an IC50 of 2 nM, showing a 300-fold window over the inhibition of PARylation in PARP1-activated HeLa cells.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

RBN-2397 is a highly selective PARP7 inhibitor against other PARPs and has been shown to have in vivo pharmacological activity with oral administration. I believe RBN-2397 is one of the best probes for evaluating the biological activity of PARP7.

(last updated: 28 Oct 2022 )