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Cat. No.: HY-157559

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KDRLKZ-2

KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (K_d = 95 nM), with an IC₅₀ of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2.

For research use only. We do not sell to patients.

Formula: C₂₃H₂₉N₃O₇
Molecular Weight:459.49

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (267 KB)

KDRLKZ-2 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Ligands for E3 Ligase Isoforms :

In Vitro

KDRLKZ-2 competes with the native SelK peptide substrate for binding to purified KLHDC2 in alphaLISA displacement assays, with an IC₅₀ of 0.068 μM^[1].
KDRLKZ-2 competes with the native SelK peptide substrate for binding to purified KLHDC2 in TR-FRET displacement assays, with an IC₅₀ of 0.1 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 459.49
Formula C₂₃H₂₉N₃O₇
SMILES

O=C(O)CN1C=C(N2C(C(C(C)CC)=CC3=C2CN(C(OCCOC)=O)CC3)=O)C=CC1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hickey CM, et al. Co-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules. Nature structural & molecular biology. 2024 Feb;31(2):311-322. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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