CRBN-6-5-5-VHL

CRBN-6-5-5-VHL : Degrader, PROTAC of CRBN

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

CRBN

Degrader (PROTAC)

~~100-1000 nM~~
Reviewer recommended concentration: 5-10 nM for measuring degradation and 50-100nM to study downstream effects

Probe Availability:

TOCRIS

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

IKZF1 (Ikaros) and IKZF3 (Aiolos) are transcription factors and neosubstrates of Cereblon. Application of CRBN-6-5-5-VHL does not result in degradation of these proteins.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a good probe that can be used to study the CRBN degradation. The in vivo properties of this molecule still need to be evaluated or improved.

(last updated: 16 Feb 2021 )

SERP Ratings

In Cell Rating

SERP Comments:

The compound is highly potent at very low nanomolar range.

(last updated: 26 Feb 2021 )

SERP Ratings

In Cell Rating

(last updated: 9 Apr 2021 )