KT-253

KT-253 : Degrader (PROTAC) of MDM2

Structure

SERP Rating

Probe KT-253 is in the process of SERP review.

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Information

MDM2

Degrader (PROTAC)

up to 100 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): The selectivity of KT-253 for MDM2 was investigated using tandem mass tag–based deep proteome profiling of approximately 9,000 human proteins. Treatment of RS4;11 ALL cells with 20 nmol/L KT-253 [10-fold 90% inhibitory concentration (IC90)] for 2, 4, and 8 hours revealed a high level of selectivity. KT-253-mediated degradation of MDM2 promotes stabilization of transcriptionally active p53 and its downstream signaling pathway.

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SERP ratings and comments

No SERP comments found for KT-253