所有图片(2)
InSolution Hh/Gli Antagonist, GANT61, 2,2ʹ-(2-(Pyridin-4-yl)dihydropyrimidine-1,3(2H,4H)-diyl) bis(methylene) bis(N,N-dimethylaniline), NSC 136476, 2-((3-(2-(Dimethylamino)benzyl)-2-(4-pyridinyl)tetrahydro-1(2H)-pyrimidinyl)methyl)-N,N-dimethylaniline
C27H35N5
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质量水平
检测方案
≥95% (HPLC)
形式
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light
运输
dry ice
储存温度
−20°C
SMILES字符串
CN(C)C1=CC=CC=C1CN2CCCN(CC3=CC=CC=C3N(C)C)C2C4=CC=NC=C4
InChI
1S/C27H35N5/c1-29(2)25-12-7-5-10-23(25)20-31-18-9-19-32(27(31)22-14-16-28-17-15-22)21-24-11-6-8-13-26(24)30(3)4/h5-8,10-17,27H,9,18-21H2,1-4H3
InChI key
KVQOGDQTWWCZFX-UHFFFAOYSA-N
一般描述
A cell-permeable hexahydropyrimidine compound that displays similar pharmacological property as, but is structurally disctinct from, GANT58 (>Cat. No. 373400). While both compounds act as downstream Hedgehog (Hh) pathway-selective blockers and target Gli-mediated gene transactivation with similar potency (IC50 ~5 µM) in SAG-stimulated Shh-L2 cells, GANT61 does exhibit better in vivo antitumor efficacy, presumably due to its superior pharmacokinetics, and only GANT61, but not GANT58, is shown to inhibit Gli DNA binding in HEK293 cells. The solid form of this compound (Cat. No. 373401) is also available.
生化/生理作用
Cell permeable: yes
Primary Target
Gli1 and Gli2
Gli1 and Gli2
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
外形
A 25 mM (2 mg/186 µL) solution of Hh/Gli Antagonist, GANT61 (Cat. No. 373401) in DMSO.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
Proceedings of the National Academy of Sciences of the United States of America, 104(20), 8455-8460 (2007-05-15)
The developmentally important Hedgehog (Hh) signaling pathway has recently been implicated in several forms of solid cancer. Current drug development programs focus on targeting the protooncogene Smoothened, a key transmembrane pathway member. These drug candidates, albeit promising, do not address
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