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Menin–KMT2A-IN-1

Menin–KMT2A-IN-1 (Compound 20) is the inhibitor for menin–KMT2A that binds to menin with an IC50 of 8 nM, and inhibits the interaction between menin and lysine methyltransferase 2A (KMT2A) . Menin–KMT2A-IN-1 inhibits hERG with an IC50 of 65 μM. Menin–KMT2A-IN-1 inhibits cell MV4-11 with an IC50 of 74 nM. Menin–KMT2A-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mouse with an orally bioavailability of 74%[1].

Product Specifications

UNSPSC

12352005

Target

Epigenetic Reader Domain; Potassium Channel

Related Pathways

Epigenetics; Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

FC1=CC=C(OC2=NN=CN=C2N3CC4(CCN(CC5(C)CC5)CC4)C3)C(C(N6C7COCC6CC7)=O)=C1

Molecular Formula

C28H35FN6O3

Molecular Weight

522.61

References & Citations

[1]Chapsal BD, et al., Design of Potent Menin-KMT2A Interaction Inhibitors with Improved In Vitro ADME Properties and Reduced hERG Affinity. ACS Med Chem Lett. 2024 Dec 31;16 (2) :224-233.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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