生物活性
UNC0631 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM, respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.
化学数据
分子量 | 635.93 |
分子式 | C37H61N7O2 |
CAS号 | 1320288-19-4 |
纯度 | >98% |
溶解性(25°C) | DMSO |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | MDA-MB-231, PC3, HCT116, 22RV1, MCF7 and IMR90 cells |
方法 | Culturing MDA-MB-231, PC3, HCT116 cells in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Treating cells with inhibitors for 48 h. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1mg/mL of MTT and incubated for 1–2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazanis solubilized in acidified isopropanol and 1% Triton. Formazan signal absorbance is measured at 570 nm and corrected for the 650 nm background. IC50s are calculated using GraphPad Prizm statistical package with sigmoidal variable slope dose response curve fit |
浓度 | ~10 μM |
处理时间 | 48 hours |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 1.5725 mL | 7.8625 mL | 15.725 mL |
5 mM | 0.3145 mL | 1.5725 mL | 3.145 mL |
10 mM | 0.1573 mL | 0.7863 mL | 1.5725 mL |