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Art. -Nr.: HY-168634

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SJ46421

SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC₅₀ of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research.
(Pink: BRD3 BD2 ligand (HY-13030); Blue: KLHDC2 ligand (HY-168536); Black: linker (HY-20797)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₂H₄₁ClN₈O₅S₂
Molecular Weight:837.41

Speicherung:

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

Data Sheet (273 KB)

SJ46421 Chemical Structure

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC₅₀ of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research^[1]. (Pink: BRD3 BD2 ligand (HY-13030); Blue: KLHDC2 ligand (HY-168536); Black: linker (HY-20797)).

IC₅₀ & Target^[1]

BRD3 BD2

987 nM (Kd)

BRD4 BD2

1020 nM (Kd)

BRD2 BD2

2090 nM (Kd)

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In Vitro

SJ46421 (0.6 μM; 0-60 seconds) promotes efficient polyubiquitylation of BRD2BD2, BRD3BD2, and BRD4BD2 via neddylated CRL2KLHDC2 in vitro^[1].
SJ46421 (0.001-10 μM; 15 minutes pre-incubation) forms a high-affinity ternary complex with neddylated CRL2_KLHDC2 and BRD3_BD2, potently inhibiting KLHDC2 substrate ubiquitylation with a K_i(app) of 7.84 nM^[1].
SJ46421 forms a highly positively cooperative ternary complex with KLHDC2SBD and BRD3BD2 (α=16) with a K_d of 19 nM, while forming only moderately cooperative complexes with BRD2BD2 (α=1.4) and BRD4BD2 (α=2.8)^[1].

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

Chemical Information

Molecular Weight 837.41
Formel C₄₂H₄₁ClN₈O₅S₂
SMILES

O=C(O)CNC(CC1=CSC(C2=CC=C3C=CC=C(OCCN4CCN(C(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)CC4)C3=C2)=N1)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

Verweise

[1]. Scott DC, et al. Principles of paralog-specific targeted protein degradation engaging the C-degron E3 KLHDC2. Nature communications. 2024 Oct 12;15(1):8829. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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SJ46421

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