1. Epigenetics
  2. Histone Demethylase
  3. INCB059872 dihydrochloride

INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia.

For research use only. We do not sell to patients.

INCB059872 dihydrochloride Chemical Structure

INCB059872 dihydrochloride Chemical Structure

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1 mg USD 350 In-stock
5 mg USD 950 In-stock
10 mg USD 1500 In-stock
25 mg USD 3000 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia[1].

IC50 & Target[1]

KDM1/LSD1

 

In Vitro

INCB059872 (25 nM; 48 hours; 293T cells) dihydrochloride increases enhancer activity and gene expression[1].
INCB059872 (25 nM; 24 hours; THP-1 cells) dihydrochloride makes THP-1 show a growth defect within one cell doubling time or approximately 3 days[1].
INCB059872 (THP-1 cells) dihydrochloride regulates PRO-seq analysis identifies genes and enhancers[1].

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

Western Blot Analysis[1]

Cell Line: 293T cells
Concentration: 250 nM
Incubation Time: 48 hours
Result: Increased enhancer activity and gene expression.
In Vivo

INCB059872 (10 mg/kg; p.o.; 0, 4, or 6 days; C57BL/6J mice) dihydrochloride makes single-cell RNA-seq revealing changes in bone marrow progenitor populations[1].

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

Animal Model: C57BL/6J mice[1]
Dosage: 10 mg/kg
Administration: p.o.; 0, 4, or 6 days
Result: Single-cell RNA-seq revealed changes in bone marrow progenitor populations.
Clinical Trial
Molecular Weight

459.45

Formula

C23H36Cl2N2O3

Appearance

Solid

Color

White to light yellow

SMILES

OC(C1(CCC1)CN2CCC(COC)(CC2)CN[C@H]3[C@@](C4=CC=CC=C4)([H])C3)=O.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

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 : 3.57 mg/mL (7.77 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1765 mL 10.8826 mL 21.7652 mL
5 mM 0.4353 mL 2.1765 mL 4.3530 mL
View the 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.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 2.1765 mL 10.8826 mL 21.7652 mL 54.4129 mL
5 mM 0.4353 mL 2.1765 mL 4.3530 mL 10.8826 mL
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INCB059872 dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
INCB059872 dihydrochloride
Cat. No.:
HY-141677A
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