Antitumor agent-101
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model[1].
Product Specifications
CAS Number
2848632-52-8
UNSPSC
12352005
Target
GLP Receptor; Histone Methyltransferase
Type
Reference compound
Related Pathways
Epigenetics; GPCR/G Protein
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/antitumor-agent-101.html
Solubility
10 mM in DMSO
Smiles
COC1=CC2=C(N=C(N(C)C(C=C)=O)N=C2NC3CCN(C)CC3)C=C1OCCCN4CCCC4
Molecular Formula
C26H38N6O3
Molecular Weight
482.62
References & Citations
[1]Feng Z, et.al. Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP. J Med Chem. 2023 Jun 22;66 (12) :8086-8102.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C
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