2. PROTAC
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  4. 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).

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KL-465

KL-465 Chemical Structure

CAS No. : 3057446-82-6

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KL-465 Related Antibodies

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Description

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

 

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.

KL-465 Related Antibodies

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.
Molecular Weight

1021.19

Formula

C56H60N8O9S
CAS No.
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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KL-465 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KL-4653057446-82-6KL465KL 465PROTACscolorectal cancerTRIM28HCT116 cellsMAGE-A3A375VHLHeLa cellsMOLM13VHL E3 ubiquitin ligaseHEK293Inhibitorinhibitorinhibit

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