| Identification | Back Directory | [Name]
1H-Indole-2-carboxamide, N-[(1S)-1-[[(4-cyanophenyl)amino]carbonyl]-3-cyclopropylpropyl]-4,5,6,7-tetrahydro-3,6,6-trimethyl-4-oxo- | [CAS]
2648855-18-7 | [Synonyms]
RK-701
1H-Indole-2-carboxamide, N-[(1S)-1-[[(4-cyanophenyl)amino]carbonyl]-3-cyclopropylpropyl]-4,5,6,7-tetrahydro-3,6,6-trimethyl-4-oxo- | [Molecular Formula]
C26H30N4O3 | [MOL File]
2648855-18-7.mol | [Molecular Weight]
446.54 |
| Chemical Properties | Back Directory | [Boiling point ]
692.6±55.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.71±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A[1]. | [in vivo]
RK-701 (20 mg/kg and 50 mg/kg; i.p.; 5 weeks, each week for 5 consecutive days) selectively increases mouse embryos ε Y-globin and significantly down-regulates the expression level of H3K9me2 in peripheral blood cells. RK-701 has low toxicity[1].
| [IC 50]
G9a: 23-27 nM (IC50) | [References]
[1] Takase S, et al. A specific G9a inhibitor unveils BGLT3 lncRNA as a universal mediator of chemically induced fetal globin gene expression. Nat Commun. 2023 Jan 12;14(1):23. DOI:10.1038/s41467-022-35404-0 |
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