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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