LD-110 trihydrochloride
LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 trihydrochloride promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 trihydrochloride inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 trihydrochloride can be used for the study of esophagus squamous cancer.
(Pink: LSD1 ligand (HY-178826); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Formula: C42H44Cl3N7O6
- Molecular Weight:849.20
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
LD-110 (1-10 μM) trihydrochloride, 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) trihydrochloride 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) trihydrochloride 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) trihydrochloride can effectively inhibit the proliferation of ESCC KYSE-30 and EC9706 cells[1].
LD-110 (3-10 μM, 48 h) trihydrochloride 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: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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Appearance Solid
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Molecular Weight 849.20
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Formula C42H44Cl3N7O6
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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.Cl.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (117.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1776 mL | 5.8879 mL | 11.7758 mL | 29.4395 mL |
| 5 mM | 0.2355 mL | 1.1776 mL | 2.3552 mL | 5.8879 mL | |
| 10 mM | 0.1178 mL | 0.5888 mL | 1.1776 mL | 2.9439 mL | |
| 15 mM | 0.0785 mL | 0.3925 mL | 0.7851 mL | 1.9626 mL | |
| 20 mM | 0.0589 mL | 0.2944 mL | 0.5888 mL | 1.4720 mL | |
| 25 mM | 0.0471 mL | 0.2355 mL | 0.4710 mL | 1.1776 mL | |
| 30 mM | 0.0393 mL | 0.1963 mL | 0.3925 mL | 0.9813 mL | |
| 40 mM | 0.0294 mL | 0.1472 mL | 0.2944 mL | 0.7360 mL | |
| 50 mM | 0.0236 mL | 0.1178 mL | 0.2355 mL | 0.5888 mL | |
| 60 mM | 0.0196 mL | 0.0981 mL | 0.1963 mL | 0.4907 mL | |
| 80 mM | 0.0147 mL | 0.0736 mL | 0.1472 mL | 0.3680 mL | |
| 100 mM | 0.0118 mL | 0.0589 mL | 0.1178 mL | 0.2944 mL |
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