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ALLO-1 Sale

目录号 : GC14749

A smoothened antagonist

ALLO-1 Chemical Structure

Cas No.:37468-32-9

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1mg
¥508.00
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5mg
¥1,380.00
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10mg
¥2,506.00
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25mg
¥5,599.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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).

Chemical Properties

Cas No. 37468-32-9 SDF
化学名 3-(4-chlorophenyl)-5-methyl-1-(phenylmethyl)-2,4-imidazolidinedione
Canonical SMILES O=C1N(C2=CC=C(Cl)C=C2)C(N(CC3=CC=CC=C3)C1C)=O
分子式 C17H15ClN2O2 分子量 314.8
溶解度 ≤20mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.1766 mL 15.8831 mL 31.7662 mL
5 mM 0.6353 mL 3.1766 mL 6.3532 mL
10 mM 0.3177 mL 1.5883 mL 3.1766 mL
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