Home NF-κB NF-κB inhibitor EN450 For research use only.

EN450

EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. It interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D that induces the ternary complex formation between UBE2D and NFKB1. It exhibits anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.

EN450 Chemical Structure

EN450 Chemical Structure

CAS: 793719-01-4

Purity & Quality Control

Batch: E157501 DMSO] 58 mg/mL] false] Ethanol] 15 mg/mL] false] Water] Insoluble] false Purity: 99.00%
99.00

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Biological Activity

Description EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. It interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D that induces the ternary complex formation between UBE2D and NFKB1. It exhibits anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
Targets
NF-κB [1]

Chemical Information & Solubility

Molecular Weight 288.75 Formula

C11H13ClN2O3S
CAS No. 793719-01-4 SDF Download EN450 SDF
Storage (From the date of receipt) Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.

In vitro
Batch:

DMSO : 58 mg/mL ( (200.86 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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