NVP-2

NVP-2 : ATP competitive inhibitor of CDK9

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe NVP-2 is in the process of SERP review.

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Information

CDK9

ATP competitive

250 to 1000 nM

DOI - 10.1038/nchembio.2538

Probe Availability:

In Vitro Validations

Uniprot ID: P50750

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 0.514 nM

Potency Assay: Cdk9/CyclinT1 IMAP

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

Target aliases:

Cyclin-dependent kinase 9, TAK, CDC2L4, CDK9, CDK9 ...

DOI Reference: 10.1038/nchembio.2538

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Exhibits selectivity for CDK9 over a panel of 468 kinases, but inhibits DYRK1B (IC50 = 350 nM), displays <90% binding to CDK7 (IC50 >10 μM) and CDK13. Shows inhibition of CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 584 nM, 706 nM, and 605 nM

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 30 Jun 2021 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Several CDK9 inhibitors are available and can be used with NVP-2 as orthogonal probe. For example, 2020 a highly selective CDK9-inhibitor (JHS-009; DOI: 10.1007/s10637-019-00868-3) was published which is suitable for in-vivo use

(last updated: 23 Sept 2024 )