PF-9366 is an allosteric inhibitor of Mat2A that binds an allosteric site on Mat2A that overlaps with the binding site for the Mat2A regulator, Mat2B, targeting S-adenosylmethionine biosynthesis, with IC50 of 420 nM and Kd of 170 nM, respectively.
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产品名称 | Transferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tipifarnib |
+++
FTase, IC50: 0.6 nM |
99%+ | |||||||||||||||||
Tolcapone |
+
COMT, Ki: 30 nM |
99%+ | |||||||||||||||||
Lonafarnib |
+++
H-ras, IC50: 1.9 nM K-ras-4B, IC50: 2.8 nM |
99%+ | |||||||||||||||||
(E)-Daporinad |
++++
NMPRTase, Ki: 0.4 nM |
99%+ | |||||||||||||||||
FTI-277 HCl |
++++
FTase, IC50: 500 pM |
98% | |||||||||||||||||
A 922500 |
++
human DGAT-1, IC50: 7 nM mouse DGAT-1, IC50: 24 nM |
98% | |||||||||||||||||
Lomeguatrib |
++
O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM |
99%+ | |||||||||||||||||
PF-04620110 |
+
DGAT1, IC50: 19 nM |
98% | |||||||||||||||||
LB42708 |
+++
FTase (N-ras), IC50: 1.2 nM FTase (K-Ras), IC50: 0.8 nM |
98% | |||||||||||||||||
GGTI298 Trifluoroacetate | ✔ | 98%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Methionine adenosyltransferase 2A (Mat2A) is responsible for the biosynthesis of S-adenosyl-L-methionine (SAM), an enzyme cofactor required for transmethylation reactions and polyamine biosynthesis. PF-9366 is an allosteric inhibitor of Mat2A with an IC50 value of 420±50nM. Pre-incubation of Mat2A with increasing concentrations of Mat2B (0–100nM) reduced the inhibitory effect of PF-9366 in a dose-dependent manner. PF-9366 inhibited SAM production in H520 cells with an IC50 value of 1.2μM. The IC50 of PF-9366 in H520 cells with Mat2B knockdown was 0.86mM. Six-hour exposure of PF-9366 inhibited SAM synthesis in Huh-7 cells with an IC50 value of 225nM[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.85mL 0.57mL 0.29mL |
14.25mL 2.85mL 1.43mL |
28.50mL 5.70mL 2.85mL |
CAS号 | 72882-78-1 |
分子式 | C20H19ClN4 |
分子量 | 350.845 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 9 mg/mL(25.65 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 |