MIV-6R

Menin-MLL PPI inhibitor of KMT2A

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

KMT2A

Menin-MLL PPI inhibitor

DOI - 10.1021/jm401868d

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q03164

Target Class: Epigenetic

Target SubClass: Protein methyltransferase

Potency: KD

Potency Value: 85 nM

Potency Assay: ITC. IC50 data were also reported (56 nM).

PDB ID for probe-target interaction (3D structure): 4GO8

Structure-activity relationship: Yes

Target aliases:

Histone-lysine N-methyltransferase 2A, TRX1, MLL1, ...

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Not available

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This compound has nice SAR and structure-based probe design. More testing for off-target activities is needed for MIV-6R, which should encompass cell-based and biochemical assays.

(last updated: 11 Sept 2016 )

SERP Ratings

In Cell Rating

(last updated: 20 Jan 2017 )

SERP Ratings

In Cell Rating

SERP Comments:

MIV-6R is a Menein-MLL PPI inhibitor with good in vitro activity. Compound inhibited cell proliferation and induced hematopoietic differentiation in MLL Leukemia cells. It also reduces the expression level of key MLL-fusion protein target genes. Therefore, the probe is useful to study MLL Leukemia cells. However, no in vivo studies are presented, and more potent inhibitors are present in the literature with a more explored profile and with in vivo activity. Additional experiments to check off-target activities should be performed.

(last updated: 18 Apr 2018 )