VinSpinIn

Inhibitor of SPIN1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe VinSpinIn is in the process of SERP review.

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Information

SPIN1

Inhibitor

Additional Data

SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q9Y657

Target Class: Transcription factor

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 ...

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).

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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 )