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AZ 12080282 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZ 12080282 dihydrochloride图片
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Hedgehog inhibitor
化学名N-(5-(1H-imidazol-2-yl)-2-methylphenyl)-4-(pyridin-2-ylmethoxy)benzamide dihydrochloride
Canonical SMILESCC1=C(NC(C2=CC=C(OCC3=NC=CC=C3)C=C2)=O)C=C(C4=NC=CN4)C=C1.Cl.Cl
分子式C23H20N4O2.2HCl
分子量457.35
溶解度Soluble in DMSO
储存条件Desiccate at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AZ 12080282 dihydrochloride is a selective inhibitor of Hh with IC50 value<0.012 μM [1]. It is also reported that AZ 12080282 also has a selective inhibition to p38α with low nanomolar potency [1].

Hedgehog (Hh) signaling plays an important role in a wide variety of developmental processes, including larval body segment development and adult appendages formation. Abnormal activation of Hh pathway may lead to developmental disease by transforming adult stem cells into cancer stem cells and also leads to cancers via increasing in Angiogenic Factors, Cyclins, anti-apoptotic genes and decreasing in apoptotic genes [2].

AZ 12080282 is a potent Hh inhibitor and is different from the other reported Hh inhibitors. When tested with Gli transcription factor reporter cell, AZ 12080282 treatment resulted in the Hh signaling pathway inhibition by using shh stimulated cell differentiation assay [1].

References:
[1].  Yang, B., et al., Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO. Bioorg Med Chem Lett, 2012. 22(14): p. 4907-11.
[2].   D'Amato, C., et al., Inhibition of Hedgehog signalling by NVP-LDE225 (Erismodegib) interferes with growth and invasion of human renal cell carcinoma cells. Br J Cancer, 2014. 111(6): p. 1168-79.