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Art. -Nr.: HY-169086

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KL-465

Name: KL-465
Brand: MedChemExpress
SKU: HY-169086
Price: 825.00 USD
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KL-465 is a MAGE-A3 PROTAC degrader that degrades MAGE-A3 in HeLa cells with a DC₅₀ of 2 μM. KL-465 inhibits the proliferation of MAGE-A3-positive cancer cells. KL-465 can be used for the research of MAGE-A3-related cancers.
(Pink: MAGE-A3 ligand (HY-169087); Blue: VHL ligand (HY-151227); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3057446-82-6
Formel: C₅₆H₆₀N₈O₉S
Molecular Weight:1021.19

Speicherung:

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

Data Sheet (277 KB)

KL-465 Chemical Structure

CAS. Nr.: 3057446-82-6

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Use of MCE Products

Fluorescent Dye

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

KL-465 is a MAGE-A3 PROTAC degrader that degrades MAGE-A3 in HeLa cells with a DC₅₀ of 2 μM. KL-465 inhibits the proliferation of MAGE-A3-positive cancer cells. KL-465 can be used for the research of MAGE-A3-related cancers^[1]. (Pink: MAGE-A3 ligand (HY-169087); Blue: VHL ligand (HY-151227); Black: linker).

IC₅₀ & Target^[1]

VHL

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In Vitro

KL-465 (0.1-10 μM; 2-24 h) induces dose- and time-dependent degradation of MAGE-A3 in HeLa cells, with a DC₅₀ of approximately 2 μM and a maximum degradation rate of around 60%, and also induces MAGE-A3 degradation in HCT116 cells^[1].
KL-465 (10 μM; 72 h) reduces the viability of MAGE-A3-positive cancer cell lines (HCT116 p53 (-), HCT116 p53 (+), A375, HeLa), while exerting minimal cytotoxicity against MAGE-A3-negative HEK293 and MOLM13 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

HeLa cells (MAGE-A3-positive cancer cell line)
Concentration:

0.1-10 μM (dose-response); 2.5-10 μM (time course)
Incubation Time:

24 h (dose-response); 2-24 h (time course)
Result:

Induced dose-dependent degradation of MAGE-A3 with a maximum degradation (Dmax) of ~60% and a DC50 of ~2 μM.
Detected degradation as early as 2 h post-treatment and sustained it through 24 h.

Western Blot Analysis^[1]

Cell Line:

HeLa cells (MAGE-A3-positive cancer cell line)
Concentration:

2.5, 10 μM
Incubation Time:

24 h
Result:

Significantly decreased MAGE-A3 protein levels at both 2.5 μM and 10 μM.
Showed no significant MAGE-A3 degradation induced by inactive control PROTAC KL633 or parent ligand MJBIA9836.

Cell Viability Assay^[1]

Cell Line:

MAGE-A3-positive cell lines (HCT116 p53(-), HCT116 p53(+), A375, HeLa); MAGE-A3-negative cell lines (HEK293, MOLM13)
Concentration:

10 μM
Incubation Time:

72 h
Result:

Reduced viability of HCT116 p53(-) cells to ~70% of DMSO control.
Reduced viability of HCT116 p53(+) cells to ~50% of DMSO control.
Reduced viability of A375 cells to ~70% of DMSO control.
Reduced viability of HeLa cells to ~60% of DMSO control.
Caused minimal changes in viability of MAGE-A3-negative HEK293 and MOLM13 cells.
Reduced cell viability to a greater extent than MJBIA9836, VHL ligand, or KL633 in MAGE-A3-positive cell lines.

Chemical Information

CAS. Nr. 3057446-82-6
Molecular Weight 1021.19
Formel C₅₆H₆₀N₈O₉S
SMILES

O=C(N1CCN(CC2=CC(C3=CC=CC4=C3C=NN4)=CC=C2OCCOCCOC5=CC(C6=C(C)N=CS6)=CC=C5CNC([C@H]7N(C([C@@H](N(CC8=C9C=CC=C8)C9=O)C(C)C)=O)C[C@H](O)C7)=O)CC1)C%10=CC=CO%10
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 (277 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]. Li K, et al. Development of Ligands and Degraders Targeting MAGE-A3. J Am Chem Soc. 2024;146(36):24884-24891. [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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100 mg

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

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KL-465

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