KL-465
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).
For research use only. We do not sell to patients.
- CAS No.: 3057446-82-6
- Formula: C56H60N8O9S
- Molecular Weight:1021.19
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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VHL |
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.
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Cell Line:HeLa cells (MAGE-A3-positive cancer cell line)
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Concentration:0.1-10 μM (dose-response); 2.5-10 μM (time course)
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Incubation Time:24 h (dose-response); 2-24 h (time course)
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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.
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Cell Line:HeLa cells (MAGE-A3-positive cancer cell line)
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Concentration:2.5, 10 μM
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Incubation Time:24 h
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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.
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Cell Line:MAGE-A3-positive cell lines (HCT116 p53(-), HCT116 p53(+), A375, HeLa); MAGE-A3-negative cell lines (HEK293, MOLM13)
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Concentration:10 μM
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Incubation Time:72 h
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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
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CAS No. 3057446-82-6
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Molecular Weight 1021.19
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Formula C56H60N8O9S
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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