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ALLO-1
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。
ALLO-1图片
CAS NO:37468-32-9
规格:98%
分子量:314.8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
SMO antagonist
CAS:37468-32-9
分子式:C17H15ClN2O2
分子量:314.8
纯度:98%
存储:Store at -20°C

Background:

IC50: 50 nM for wile type Smo


ALLO-1 is a SMO antagonist.


Hedgehog (Hh) proteins are important development regulators that bind the cell-surface protein, which allows the activation of a GPCR-like receptor, Smoothened (SMO). In vertebrates, the SMO activation finally results in the activation of the zinc-finger transcription factors of the Gli family. In addition, the overactivation of SMO may lead to certain cancers.


In vitro: Previous study found that ALLO-1 and its close analog ALLO-2 could inhibit Smo agonist Hh-Ag 1.5-induced luciferase expression in TM3-Gli-Luc cells. The potency of ALLO-1 did not change when either low dose or high dose of Hh-Ag 1.5 was used, in contrast to other known Smo antagonists that are strong SAG or Hh-Ag 1.5 competitors. Moreover, it was found that in contrast to GDC-0449, both ALLO-1 and ALLO-2 inhibited wild-type and the D477G mutant with only around2-fold shift in IC50, indicating that the D477G mutation did not significantly interfere with the binding of ALLO-1 and ALLO-2 to Smo. In addition, ALLO-1 as well as ALLO-2 were able to inhibit both wild-type and D473H mutant human SMO with similar potencies [1].


In vivo: Up to now, there is no animal in vivo data reported.


Clinical trial: So far, no clinical study has been conducted.


Reference:
[1] Tao, H. ,Jin, Q.,koo, D.I., et al. Small molecule antagonists in distinct binding modes inhibit drug-resistant mutant of smoothened. Chemistry & Biology 18, 432-437 (2011).