1. Epigenetics
  2. Histone Demethylase
  3. INCB059872 TFA

INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 TFA can be used for the research of myeloid leukemia.

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

INCB059872 TFA

INCB059872 TFA Chemical Structure

CAS No. : 1802909-50-7

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Description

INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 TFA can be used for the research of myeloid leukemia[1].

IC50 & Target[1]

LSD1

 

In Vitro

INCB059872 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b[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 (p.o.) TFA can significantly prolong the median survival time of mice with MLL-AF9-expressing leukemia, induce the differentiation of primitive leukemic cells in mice, reduce the formation of primitive cell colonies, and restore hematological clinical indicators to the levels observed in normal non-leukemic mice[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

500.55

Formula

C25H35F3N2O5

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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 TFA
Cat. No.:
HY-141677C
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