Биологическая активность
F5446 is a SUV39H1 ингибитор. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.
Оригинал на английском
F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.
Химические свойства
- CAS №
- 2304465-89-0
- Брутто-формула
- C₂₆H₁₇ClN₂O₈S
- Мол. масса
- 552.94 г/моль
- SMILES
- O=C(C1=CNC2=C1C3=C(N(S(=O)(C4=CC=C(Cl)C=C4)=O)C(C(OC)=O)=C3)C(C2=O)=O)OCC5=CC=CC=C5
- Синонимы
- F5446; F 5446; F-5446
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 0°C (short term), -20°C (long term), desiccated
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.