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).
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- Formule: C42H41N7O6
- Masse moléculaire:739.82
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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.
Chemical Information
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Masse moléculaire 739.82
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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