| CAS |
No.330829-30-6 |
| 英文名称 |
MRT-10 |
| 分子式 |
C24H23N3O5S |
| 分子量 |
465.52 |
| 溶解性 |
Soluble in DMSO ≥10mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD02734587 |
| SMILES |
COC1=CC(=CC(=C1OC)OC)C(=O)NC(=S)NC2=CC=CC(=C2)NC(=O)C3=CC=CC=C3 |
| InChIKey |
KVQVEZQDNHMQJV-UHFFFAOYSA-N |
| InChI |
InChI=1S/C24H23N3O5S/c1-30-19-12-16(13-20(31-2)21(19)32-3)23(29)27-24(33)26-18-11-7-10-17(14-18)25-22(28)15-8-5-4-6-9-15/h4-14H,1-3H3,(H,25,28)(H2,26,27,29,33) |
| PubChem CID |
1139102 |
| 靶点 |
Smo |
| 通路 |
Hedgehog;Stem Cells |
| 背景说明 |
MRT-10是一种七跨膜平滑受体 (Smo) 拮抗剂,可用于癌症研究。 |
| 生物活性 |
MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2]. |
| In Vitro |
MRT-10 inhibits the Smo-induced IP accumulation in a dosedependent manner (IC50=2.5 μM) in HEK293 cells[1].MRT-10 (10-9-10-5 M; 2 h) blocks Bodipy-cyclopamine (5 nM; 2 h) binding to cells expressing mouse Smo in a dosedependent manner with an IC50=0.5 μM[1].MRT-10 (10-9-10-5 M; 40 h) inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with an IC50=0.64 μM[1].MRT-10 (10-9-10-5 M; 6 days) inhibits the SAG-induced (0.1 μM) alkaline phosphatase (AP) activity with an IC50=0.90 μM ) in C3H10T1/2 cells[1]. |
| 数据来源文献 |
[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. |
| 规格 |
1mg 5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
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