LD-110 trihydrochloride
LD-110 trihydrochloride is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 trihydrochloride acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 trihydrochloride induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 trihydrochloride inhibits tumor growth in the KYSE-150 xenograft model. LD-110 trihydrochloride can be used in research related to esophageal squamous cell carcinoma.
(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)
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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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
Description
IC50 & Target
[1]|
LSD1 0.44 μM (DC50, in KYSE-150 cells) |
LSD1 1.18 μM (DC50, in KYSE-30 cells) |
LSD1 1.24 μM (DC50, in EC9706 cells) |
In Vitro
LD-110 (1-10 μM) trihydrochloride effectively degrades LSD1 protein in a dose-dependent manner in KYSE-150 cells[1].
LD-110 (10 μM; 6-72 h) trihydrochloride degrades LSD1 and increases H3K4me2 levels in KYSE-150, KYSE-30, and EC9706 ESCC cells in a time-dependent manner[1].
LD-110 (48 h) trihydrochloride treatment significantly increases H3K4me2 levels in KYSE-150, KYSE-30, and EC9706 ESCC cells[1].
LD-110 (0.1-30 μM; 48 h) trihydrochloride potently and dose-dependently degrades LSD1 and induces H3K4me2 accumulation in KYSE-150, KYSE-30, and EC9706 esophageal squamous cell carcinoma cells[1].
LD-110 trihydrochloride specifically degrades LSD1 in KYSE-150 cells without affecting the levels of other components of the LSD1 complex[1].
LD-110 (72 h) trihydrochloride effectively inhibits the growth of KYSE-150, KYSE-30, and EC9706 ESCC cells with low micromolar IC50 values[1].
LD-110 (1-10 μM; 10-14 days) trihydrochloride effectively inhibits clonogenic survival of KYSE-30 and EC9706 cells[1].
LD-110 (3-10 μM; 48 h) trihydrochloride induces apoptosis in KYSE-30 and EC9706 esophageal squamous cell carcinoma cells in a dose-dependent manner[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, EC9706
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Concentration:10 μM
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Incubation Time:6, 12, 24, 48 and 72 h
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Result:Effectively reduced LSD1 protein levels after 24-48 h of treatment and achieved near-complete depletion of LSD1 at 48-72 h.
Caused the accumulation of H3K4me2.
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Cell Line:KYSE-150, KYSE-30, EC9706
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Concentration:0.1, 0.3, 1, 3, 10, 30 μM
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Incubation Time:48 h
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Result:Caused dose-dependent degradation of LSD1 with DC50 values of 0.44 μM in KYSE-150, 1.18 μM in KYSE-30, and 1.24 μM in EC9706 cells.
Caused dose-dependent accumulation of H3K4me2.
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Cell Line:KYSE-30, EC9706
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Concentration:1, 3 μM (KYSE-30); 3, 10 μM (EC9706)
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Incubation Time:10-14 days
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Result:Effectively suppressed the colony formation of ESCC cells in a dose-dependent manner.
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Cell Line:KYSE-30, EC9706
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Concentration:3, 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.
Induced dose-dependent cleavage of both PARP and caspase-3.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, age- and weight-matched)[1]
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Dosage:30 and 100 mg/kg
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Administration:i.p.; once daily; 24 days
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Result:Dose-dependently inhibited tumor growth at 30 and 100 mg/kg without affecting body weight.
Reduced LSD1 protein levels in tumor tissues at 100 mg/kg without causing morphological changes in major organs.
Suppressed in vivo tumor growth at 100 mg/kg without toxic effects on body weight, whereas LI-1 was largely ineffective at the same dose regimen.
Achieved tumor concentrations of 437 ng/g at 30 mg/kg and 946 ng/g at 100 mg/kg.
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
In Vitro:
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 |
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| 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 |
LD-110 trihydrochloride Related Classifications
HY-178825B Related Classifications
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