所有图片(1)
别名:
7-(4-Chlorobenzyl)-1,3-dioxohexahydroimidazo[1,5-a]pyrazin-2(3H)-yl 2,3-dihydro-4Hbenzo[b][1,4]oxazine-4-carboxylate
经验公式（希尔记法）:
C22H21ClN4O5
推荐产品
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
O=C(ON(C(N1C2CN(CC1)CC3=CC=C(C=C3)Cl)=O)C2=O)N4C5=CC=CC=C5OCC4
生化/生理作用
ABC99 is an N-hydroxyhydantoin (NHH) carbamate-based irreversible, potent and selective inhibitor against the serine hydrolase activity of the Wnt-deacylating enzyme NOTUM (IC50 = 13 nM against NOTUM-mediated labeling of fluorophosphonate (FP) probe), an enzyme that reverses the posttranslational O-linked palmitoleate modification of Wnt proteins. ABC99 prevents NOTUM-mediated negative regulation against Wnt3A-dependent cellular signaling (EC50 = 89 nM by HEK293T TOPflash reporter assay) with excellent selectivity over 65 other serine hydrolases, including PPT1.
Inhibition of NOTUM has therapeutic use in treating degenerative diseases including osteopenia and osteoporosis.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Selective irreversible inhibitors of the Wnt-deacylating enzyme NOTUM developed by activity-based protein profiling
Suciu RM, et al.
ACS Medicinal Chemistry Letters, 9(6), 563-568 (2018)
Mariyan J Jeyarajah et al.
Proceedings of the National Academy of Sciences of the United States of America, 119(49), e2203071119-e2203071119 (2022-11-29)
Remodeling of the uterine vasculature by invasive extravillous trophoblasts (EVTs) is a critical aspect of human placentation. Insufficient EVT invasion can lead to severe obstetrical complications like preeclampsia, intrauterine growth restriction, and preterm birth. Glial cells missing-1 (GCM1) is a
Radu M Suciu et al.
ACS medicinal chemistry letters, 9(6), 563-568 (2018-06-26)
Wnt proteins are secreted morphogens that play critical roles in embryonic development and tissue remodeling in adult organisms. Aberrant Wnt signaling contributes to diseases such as cancer. Wnts are modified by an unusual O-fatty acylation event (O-linked palmitoleoylation of a
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