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Merck
CN
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文件

373403

Sigma-Aldrich

Hh/Gli Antagonist, GANT61

InSolution, ≥95%

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别名:
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
经验公式(希尔记法):
C27H35N5
分子量:
429.60
MDL编号:
UNSPSC代码:
51111800
NACRES:
NA.77

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

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


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Matthias Lauth et al.
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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