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EZH2-IN-14

EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3) . EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1[1].

Product Specifications

CAS Number

[1979157-17-9]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ezh2-in-14.html

Purity

99.62

Solubility

DMSO : 125 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=CC(C2=CC=C(N3CCN(C(C)C)CC3)N=C2)=CC4=C1C=NN4C(C)C)NCC5=C(C)C=C(C)NC5=O

Molecular Formula

C31H39N7O2

Molecular Weight

541.69

References & Citations

[1]Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16 (2) :214-222.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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