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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3057446-82-6
- 分子式: C56H60N8O9S
- 分子量:1021.19
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 3057446-82-6
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分子量 1021.19
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
KL-465 関連分類
HY-169086 関連分類
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