MRT-10

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Chemical Structure| 330829-30-6 同义名 : -
CAS号 : 330829-30-6
货号 : A1209369
分子式 : C24H23N3O5S
纯度 : 97%
分子量 : 465.522
MDL号 : MFCD02734587
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(225.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 MRT-10 is a seven-transmembrane receptor smoothened (smo) antagonist with an IC50 value of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the Bodipycyclopamine binding site. MRT-10 can be used in cancer research[1][2].In HEK293 cells, MRT-10 inhibited Smo-induced IP accumulation in a dose-dependent manner with an IC50 value of 2.5 μM. MRT-10 blocked the binding of Bodipy-cyclopamine (5 nM; 2 h) to the expressed mice at a concentration of 10-9-10-5M for 2 h in a dose-dependent manner, binding to cells expressing mouse Smo with an IC50 value of 0.5 μM. Treatment for 40h, MRT-10 inhibited ShhN signalling in Shh-light2 cells in a dose-dependent manner with an IC50 value of 0.64 μM. Treatment for 6 days, MRT-10 inhibited SAG-induced (0.1 μM) alkaline phosphatase (AP) activity in C3H10T1/2 cells with an IC50 value of 0.90 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.48mL

4.30mL

2.15mL
参考文献

[1]Manetti F, et al. Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists. Mol Pharmacol. 2010 Oct;78(4):658-65.

[2]Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012 Feb 23;55(4):1559-71.