VinSpinIn

VinSpinIn : Inhibitor of SPIN1, SPIN2A, SPIN2B, SPIN3, SPIN4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 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.

Probe VinSpinIn is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

SPIN1
SPIN2A
SPIN2B
SPIN3
SPIN4

Inhibitor

Additional Data

SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: Q9Y657

Target Class: Epigenetic

Target SubClass: Chromatin Regulator

Potency: Kd, IC50

Potency Value: 9.9 nM. (Kd); 33 nM (IC50)

Potency Assay: AlphaScreen, SYPRO Orange thermal shift assay, ITC

PDB ID for probe-target interaction (3D structure): 6I8B

Structure-activity relationship: yes

Target aliases:

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

DOI Reference: 10.1021/acs.jmedchem.9b00562

Uniprot ID: Q9Y657

Target Class: Epigenetic

Target SubClass: Chromatin Regulator

Potency: ΔTm

Potency Value: 13.17

Potency Assay: Thermal Shift 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.9b00562

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): ITC, DSF

Probe Selectivity in Vitro:

Selectivity was assessed by ITC on four SPIN subfamily members. SPIN1-49–262 (9.9 nM), SPIN1-26–262 (111.1 nM), SPIN2B-45–258 (46.1 nM), SPIN3-27–258 (131.1 nM), SPIN4-36–249 (18.1 nM). VinSpinIn was screened against a panel of methyl binding domains (MBDs) using the thermal shift assay (DSF). No significant thermal shift was observed for any of the MBDs screened A Scintillation Proximity Assay (SPA) was employed to screen VinSpinIn against a panel of methyltransferases and IC50s were determine for selected targets. The lowest IC50 of VinSpinIn (PRMT4) was approximately 300 times greater than the AlphaScreen IC50 on Spin1 (30 nM).

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This compound is quite specific to the Spin family proteins, therefore it will be helpful for studying cellular functions of the family. Especially the control compound with similar structure and same molecular weight but without activity will greatly contribute to discuss the phenomena when incubated with the inhibitor. However, you should obtain background general data such as if the compounds have non-selective toxicity, before conducting pharmacological examinations.

(last updated: 20 Mar 2021 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a well characterised compound, but both the active and inactive compounds displayed toxicity, implying off-target effects. Despite significant effort, the toxicity issues relating to this series could not be resolved.

(last updated: 23 Sept 2024 )