MS8535

MS8535 : Inhibitor of SPIN1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe MS8535 is in the process of SERP review.

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Information

SPIN1

Inhibitor

up to 5 uM

In Vitro Validations

Uniprot ID: Q9Y657

Target Class: Epigenetic

Target SubClass: Chromatin regulator

Potency: Kd

Potency Value: 30 ± 2 nM

Potency Assay: ITC assay for SPIN1

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

Target aliases:

Spindlin-1, SPIN, OCR, SPIN1, SPIN1_HUMAN, Spindli ...

DOI Reference: 10.1021/acs.jmedchem.4c00121

Uniprot ID: Q9Y657

Target Class: Epigenetic

Target SubClass: Chromatin regulator

Potency: IC50

Potency Value: 202 ± 11 nM

Potency Assay: FP assay

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

Target aliases:

Spindlin-1, SPIN, OCR, SPIN1, SPIN1_HUMAN, Spindli ...

DOI Reference: 10.1021/acs.jmedchem.4c00121

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): MS8535 showed very weak binding to G9a and GLP in ITC studies. Selectivity profile of MS8535 in a panel of 38 epigenetic targets, including G9a and GLP, found that MS8535 did not significantly inhibit the enzymatic activity of these epigenetic targets (<20% of inhibition at 1 μM). MS8535 was >18-fold selective for SPIN1 over several other SPIN family members, such as SPIN2B (Kd = 0.56 μM), SPIN3 (Kd = 1.4 μM), and SPIN4 (Kd = 0.71 μM) as measured by ITC.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

There is no PK data reported for this compound, only a total concentration vs time graph for mouse IP administration. Without any fraction unbound data and PK parameters, it is impossible to know what unbound exposure there will be in the mouse. This compound may well be suitable, but more data is needed to understand if this is the case.

(last updated: 3 Jun 2024 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is an interesting new compound that inhibits SPIN1 with potency and selectivity in a limited panel of epigenetic targets. Before its wide application as a chemical probe, it would be desirable to have unbiased data on potential off-targets in a cellular context, e.g. by chemical proteomics or thermal proteome profiling.

(last updated: 17 Jun 2024 )