Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-

Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  HSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with IC50 value <0.05 nM. hSMG-1 inhibitor 11e exhibits 900-fold selectivity for hSMG-1 over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50 of 61 nM and 92 nM) and CDK1/CDK2 (IC50 of 32 μM and 7.1 μM).

• in vitro

  HSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment.

• target

  mTOR 45 nM (IC 50 )

  PI3Kα 61 nM (IC 50 )

  PI3Kγ 92 nM (IC 50 )

  CDK1 32 μM ( IC 50 )

  CDK2 7.1 μM (IC 50 )

  hSMG-1 <0.05 nM (IC 50 )

Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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