country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-178825B

Copy Link Print Information

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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₂H₄₄Cl₃N₇O₆
Molecular Weight:849.20

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

LD-110 trihydrochloride Chemical Structure

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: LSD1 ligand (HY-178826); Blue: Cereblon ligand (HY-14658); Black: linker).

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)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

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.

Western Blot Analysis^[1]

Cell Line:

KYSE-150, KYSE-30, EC9706
Concentration:

10 μM
Incubation Time:

6, 12, 24, 48 and 72 h
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.

Western Blot Analysis^[1]

Cell Line:

KYSE-150, KYSE-30, EC9706
Concentration:

0.1, 0.3, 1, 3, 10, 30 μM
Incubation Time:

48 h
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.

Cell Proliferation Assay^[1]

Cell Line:

KYSE-30, EC9706
Concentration:

1, 3 μM (KYSE-30); 3, 10 μM (EC9706)
Incubation Time:

10-14 days
Result:

Effectively suppressed the colony formation of ESCC cells in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

KYSE-30, EC9706
Concentration:

3, 10 μM
Incubation Time:

48 h
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

LD-110 (30-100 mg/kg; i.p.; once daily; 24 days) trihydrochloride effectively suppresses tumor growth in a KYSE-150 xenograft model without obvious toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (male, age- and weight-matched)^[1]
Dosage:

30 and 100 mg/kg
Administration:

i.p.; once daily; 24 days
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

Appearance Solid
Molecular Weight 849.20
Formel C₄₂H₄₄Cl₃N₇O₆
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1776 mL

5.8879 mL

11.7758 mL

5 mM

0.2355 mL

1.1776 mL

2.3552 mL

10 mM

0.1178 mL

0.5888 mL

1.1776 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Zhuo J, et al. Discovery of LD-110 as an Effective LSD1 PROTAC Degrader for the Treatment of Esophagus Squamous Cancer. Journal of medicinal chemistry. 2025 Oct 23;68(20):21860-21877. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

LD-110 trihydrochloride

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

In Vitro

In Vivo

Chemical Information

Lösungsmittel & Löslichkeit

In Vitro:

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table