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EPZ033294

EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM) . SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T[1].

Product Specifications

CAS Number

1887195-17-6

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/epz033294.html

Smiles

O=C(C1=CN(C2CC2)N=N1)NC3CN(C3)CC4=CN(CC5=CC=C(C=C5)Cl)N=C4

Molecular Formula

C20H22ClN7O

Molecular Weight

411.89

References & Citations

[1]Michael J, et al. Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. PLOS ONE. 2018 Jun 1;13 (6) :e0197372.|[2]Edoardo Fabini, et al. Small-molecule inhibitors of lysine methyltransferases SMYD2 and SMYD3: current trends. Medicinal Chemistry. 2019 Apr;11 (8) :901-921.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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