2. Epigenetics
  3. Histone Demethylase
  4. INCB059872

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

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

INCB059872 Chemical Structure

INCB059872 Chemical Structure

CAS No. : 1802909-49-4

Size Price Stock Quantity
1 mg USD 350 In-stock
5 mg USD 950 In-stock
10 mg USD 1500 In-stock
25 mg USD 3000 In-stock
50 mg USD 4800 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

KDM1/LSD1

 

In Vitro

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

INCB059872 Related Antibodies

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) 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: 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

386.53

Formula

C23H34N2O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (517.42 mM; Need ultrasonic; 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 2.5871 mL 12.9356 mL 25.8712 mL
5 mM 0.5174 mL 2.5871 mL 5.1742 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (12.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (12.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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. 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 2.5871 mL 12.9356 mL 25.8712 mL 64.6780 mL
5 mM 0.5174 mL 2.5871 mL 5.1742 mL 12.9356 mL
10 mM 0.2587 mL 1.2936 mL 2.5871 mL 6.4678 mL
15 mM 0.1725 mL 0.8624 mL 1.7247 mL 4.3119 mL
20 mM 0.1294 mL 0.6468 mL 1.2936 mL 3.2339 mL
25 mM 0.1035 mL 0.5174 mL 1.0348 mL 2.5871 mL
30 mM 0.0862 mL 0.4312 mL 0.8624 mL 2.1559 mL
40 mM 0.0647 mL 0.3234 mL 0.6468 mL 1.6170 mL
50 mM 0.0517 mL 0.2587 mL 0.5174 mL 1.2936 mL
60 mM 0.0431 mL 0.2156 mL 0.4312 mL 1.0780 mL
80 mM 0.0323 mL 0.1617 mL 0.3234 mL 0.8085 mL
100 mM 0.0259 mL 0.1294 mL 0.2587 mL 0.6468 mL
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INCB059872 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.

Keywords:

INCB0598721802909-49-4INCB 059872INCB-059872Histone DemethylasepotentselectiveirreversibleLysine-SpecificDemethylasemyeloidleukemiaInhibitorinhibitorinhibit

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