Antitumor agent-101

• Description :

  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].

• 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

• CAS Number :

  [2848632-52-8]