2. Epigenetics
  3. Epigenetic Reader Domain
  4. Menin-MLL-IN-37

Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC50 of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML).

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

Menin-MLL-IN-37

Menin-MLL-IN-37 Chemical Structure

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Menin-MLL-IN-37 Related Antibodies

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Description

Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC50 of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

Menin-MLL

820.50 nM (IC50)

In Vitro

Menin-MLL-IN-37 (Compound A13) potently inhibits the proliferation of MLL-rearranged (MV4-11, MOLM-13), DNMT3A/NPM1-mutated (OCI-AML3) and other leukemia cell lines (THP-1, HL-60, K562), with IC50 values of 0.379, 0.838, 0.763, 1.618, 1.179 and 2.653 μM[1].
Menin-MLL-IN-37 (1-2 μM; 7 days) induces differentiation of MV4-11 and MOLM-13 leukemia cells, resulting in increased surface expression levels of CD11b[1].

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

Menin-MLL-IN-37 Related Antibodies

Cell Differentiation Assay[1]

Cell Line: MV4-11, MOLM-13 leukemia cell lines
Concentration: 1000 nM, 2000 nM
Incubation Time: 7 days
Result: Induced a significant increase in the percentage of CD11b-positive cells in MV4-11 cell line.
Induced a significant increase in the percentage of CD11b-positive cells in MOLM-13 cell line.
Parmacokinetics
Species Dose Route Tmax T1/2 Cmax AUC0-t AUC0-∞ MRT0-t Vz/F CL/F
Mice[1] 20 mg/kg i.g. 1.67 h 2.43 h 537.00 ng/mL 2241.09 ng·h/mL 2379.51 ng·h/mL 3.59 h 30499.24 mL/kg 147.32 mL/min/kg
In Vivo

Menin-MLL-IN-37 (Compound A13) (20 mg/kg; i.g.; single dose) exhibits favorable oral pharmacokinetic properties in mice, with rapid absorption and high bioavailability[1].

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

638.77

Formula

C29H37F3N6O3S2
SMILES

FC(F)(F)CC1=CC2=C(NC3CCN(CC4CCN(C5=CC=C(S(=O)(N6CCOCC6)=O)C=C5)CC4)CC3)N=CN=C2S1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Menin-MLL-IN-37 Related Classifications

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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:

Menin-MLL-IN-37Epigenetic Reader DomainMLL-rearranged leukemia cellsDNMT3A/NPM1-mutated leukemia cellsMOLM-13 cellsMV4-11 cellsOCI-AML3 cellsMLL proteinshuman menin proteinacute myeloid leukemia cellsMenin-MLL protein complexmeninInhibitorinhibitorinhibit

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