LD-110
LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer.
(Pink: LSD1 ligand (HY-178826); Blue: Cereblon ligand (HY-14658); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C42H41N7O6
- 分子量:739.82
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
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生物活性
LD-110 (1-10 μM), with a linker containing four methylene groups, demonstrates good degradation activity, achieving degradation rates of 65, 70, and 84% against the LSD1 protein at concentrations of 1, 3, and 10 μM, respectively[1].
LD-110 (0.1-30 μM, 6-72 h) effectively and dose-dependently degrades LSD1 protein, achieving near-complete depletion within 48-72 hours with DC50 values of 0.44, 1.18, and 1.24 μM in KYSE-150, KYSE-30, and EC9706 ESCC cells, respectively; this degradation is highly specific with minimal effect on CoREST/HDAC1/HDAC2 levels, and consequently leads to a potent 2 to 7-fold accumulation of H3K4me2[1].
LD-110 (72 h) effectively suppresses the growth of ESCC cells with half-maximal inhibitory concentration (IC50) values of 3.94, 3.35, and 3.08 μM in KYSE-150, KYSE-30, and EC9706, respectively[1].
LD-110 (3-10 μM, 10-14 days) can effectively inhibit the proliferation of ESCC KYSE-30 and EC9706 cells[1].
LD-110 (3-10 μM, 48 h) dose-dependently induces both early-stage and late-stage apoptosis and causes cleavage of PARP and caspase-3 in KYSE-30 and EC9706 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-150, KYSE-30, and EC9706 ESCC cells
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Concentration:10 μM
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Incubation Time:6 h, 12 h, 24 h, 48 h, 72 h
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Result:Effectively reduced the LSD1 protein levels after 24-48 h treatment, achieving near-complete depletion of LSD1 at 48−72 h, consequently causing the accumulation of H3K4me2.
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Cell Line:KYSE-150, KYSE-30, and EC9706 ESCC cells
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Concentration:0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
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Incubation Time:48 h
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Result:Caused the dose-dependent degradation of LSD1 with DC50 values of 0.44, 1.18, and 1.24 μM in the KYSE-150, KYSE-30, and EC9706, respectively.
Caused accumulation of H3K4me2, which also occurred in a dose-dependent manner.
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Cell Line:KYSE-30, EC9706 ESCC cells
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Concentration:3 μM, 10 μM
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Incubation Time:10-14 days
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Result:Significantly reduced the number of clones formed in ESCC KYSE-30 and EC9706 cells in a dose-dependent manner.
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Cell Line:KYSE-30 cells, EC9706 ESCC cells
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Concentration:3 μM, 10 μM
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Incubation Time:48 h
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Result:Induced both early-stage and late-stage apoptosis in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KYSE-150 cells were injected into both flanks of the male BALB/c nude mice[1].
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Dosage:30 mg/kg, 100 mg/kg
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Administration:I.p., once daily for 24 days
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Result:Dose-dependently inhibited the tumor growth at both 30 and 100 mg/ kg via intraperitoneal administration without any effect on body weight.
At a dose of 100 mg/kg also effectively reduced the levels of LSD1 protein in the tumor tissues harvested and collected at the end of the study without causing any morphological changes of major organs, including heart, liver, spleen, lung, and kidney.
化学情報
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分子量 739.82
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分子式 C42H41N7O6
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SMILES
O=C(NCCCCNC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)C4=CC=C(C5=NC=C(OCC6CCNCC6)C=C5C7=CC=C(C#N)C=C7)C=C4
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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)
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