LD-110
LD-110 is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 inhibits tumor growth in the KYSE-150 xenograft model. LD-110 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: C42H41N7O6
- Molecular Weight:739.82
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Storage:
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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Biological Activity
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Chemical Information
- 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) effectively degrades LSD1 protein in a dose-dependent manner in KYSE-150 cells[1].
LD-110 (10 μM; 6-72 h) 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) treatment significantly increases H3K4me2 levels in KYSE-150, KYSE-30, and EC9706 ESCC cells[1].
LD-110 (0.1-30 μM; 48 h) 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 specifically degrades LSD1 in KYSE-150 cells without affecting the levels of other components of the LSD1 complex[1].
LD-110 (72 h) 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) effectively inhibits clonogenic survival of KYSE-30 and EC9706 cells[1].
LD-110 (3-10 μM; 48 h) 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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Molecular Weight 739.82
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LD-110 Related Classifications
HY-178825 Related Classifications
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