Биологическая активность
YTHDC1 ингибитор 40 is a мощный, селективный m6A reader YTHDC1 ингибитор with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) клетка lines THP-1, MOLM-13, and NOMO-1.YTHDC1 ингибитор 40 exhibits antiproliferative activity against THP-1 (GI50 = 3.2 μM), MOLM-13 (5.6 μM) and NOMO-1 (8.2 μM), respectively. YTHDC1 ингибитор 40 displays IC50 values of 89, 60, and 83 μM against YTHDF1, YTHDF2, and YTHDF3, respectively, indicating a 200-fold selectivity.YTHDC1 ингибитор 40 does not display significant inhibition of a panel of 58 protein kinases.YTHDC1 ингибитор 40 (2.5-10 uM) induces apoptosis in THP-1 клетка line after 24 h treatment.YTHDC1 ингибитор 40 is a tool compound for studying the role of YTHDC1 in AML.
Оригинал на английском
YTHDC1 inhibitor 40 is a potent, selective m6A reader YTHDC1 inhibitor with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) cell lines THP-1, MOLM-13, and NOMO-1.YTHDC1 inhibitor 40 exhibits antiproliferative activity against THP-1 (GI50 = 3.2 μM), MOLM-13 (5.6 μM) and NOMO-1 (8.2 μM), respectively. YTHDC1 inhibitor 40 displays IC50 values of 89, 60, and 83 μM against YTHDF1, YTHDF2, and YTHDF3, respectively, indicating a 200-fold selectivity.YTHDC1 inhibitor 40 does not display significant inhibition of a panel of 58 protein kinases.YTHDC1 inhibitor 40 (2.5-10 uM) induces apoptosis in THP-1 cell line after 24 h treatment.YTHDC1 inhibitor 40 is a tool compound for studying the role of YTHDC1 in AML.
Химические свойства
- CAS №
- 2995344-53-9
- Брутто-формула
- C₁₃H₁₁Cl₂N₅
- Мол. масса
- 308.17 г/моль
- SMILES
- CNC1=NC(Cl)=NC2=C(CC3=CC=CC(Cl)=C3)NN=C21
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО Publication: [1]. František Zálešák, et al. Structure-Based Design of a Potent and Selective YTHDC1 Ligand. J Med Chem. 2024 Jun 13;67(11):9516-9535.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.