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经验公式(希尔记法):
C15H14N2
化学文摘社编号:
分子量:
222.29
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C15H14N2/c1-11-3-6-13(7-4-11)14-10-17-9-12(2)5-8-15(17)16-14/h3-10H,1-2H3
SMILES string
CC1=CC=C(C2=CN3C=C(C=CC3=N2)C)C=C1
InChI key
AWEWSJJCANQFRB-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Highly potent and selective H3K4 demethylase KDM5A (JARID1A) inhibitor that improves iPSC reprogramming efficiency of human fibroblasts via OCT4 induction.
O4I3 is a highly potent and KDM5A (JARID1A) subtype-selective H3K4 demethylase KDM5 inhibitor (KDM5A IC50 = 0.15 nM vs KDM5B/C/D IC50 = 125.2/9.76/4.7 nM, KDM4 IC50 = 249 nM, LSD1 IC50 >100 μM) that effectively induces OCT4 expresson and improves OSKM-induced pluripotent stem cell (iPSC) reprogramming efficiency of human primary fibroblasts (50 nM) by preventing KDM5A from interfering with H3K4Me3 enrichment at the OCT4 promoter. O4I3 promotes hPSC homeostasis and represses cellular differentiation, increasing hPSCs viability up to 4-fold at a low 10 nM concentration when compared with Rock inhibitor Y-27632 treatment at 10 μM.
存储类别
11 - Combustible Solids
wgk
WGK 3
Yasamin Dabiri et al.
iScience, 12, 168-181 (2019-01-28)
Pioneering human induced pluripotent stem cell (iPSC)-based pre-clinical studies have raised safety concerns and pinpointed the need for safer and more efficient approaches to generate and maintain patient-specific iPSCs. One approach is searching for compounds that influence pluripotent stem cell
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