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产品名称 | ERK ↓ ↑ | ERK1 ↓ ↑ | ERK2 ↓ ↑ | ERK5 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
DEL-22379 |
+
ERK, IC50: 0.5 μM |
+
ERK, IC50: 0.5 μM |
98% | ||||||||||||||||
Pluripotin |
++
ERK1, Kd: 98 nM |
RasGAP | 98+% | ||||||||||||||||
FR 180204 |
+
ERK1, Ki: 0.31 μM |
++
ERK2, Ki: 0.14 μM |
98% | ||||||||||||||||
Ravoxertinib |
+++
ERK1, IC50: 1.1 nM |
++++
ERK2, IC50: 0.3 nM |
99%+ | ||||||||||||||||
SCH772984 |
+++
ERK1, IC50: 4 nM |
++++
ERK2, IC50: 1 nM |
99%+ | ||||||||||||||||
Temuterkib |
+++
ERK1, IC50: 5 nM |
+++
ERK2, IC50: 5 nM |
99%+ | ||||||||||||||||
VX-11e |
+++
ERK2, Ki: <2 nM |
99%+ | |||||||||||||||||
Ulixertinib |
++++
ERK2, IC50: <0.3 nM |
99%+ | |||||||||||||||||
XMD17-109 |
++
ERK5, IC50: 162 nM |
99%+ | |||||||||||||||||
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 | SKI V is a highly potent noncompetitive inhibitor of non-lipid sphingosine kinase (SPHK; SK), with an IC50 of 2 μM for GST-hSK. Additionally, SKI V exhibits potent inhibition of PI3K, with an IC50 of 6 μM for hPI3K. It effectively reduces the formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V demonstrates apoptotic induction and displays significant antitumor activity[1][2]. |
体内研究 | SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly reduces tumor growth (>50% decreased at day 18) compared to control animals[1]. |
体外研究 | SKI V exhibits low activity against ERK2 (IC50 of 80 μM for hERK2) and it does not inhibit PKC-α[1]. SKI V (10 μM; 24-hour treatment) suppresses cancer cell proliferation and triggers apoptosis[1]. SKI V (0.2, 1, 5 μM; pretreated for 1 hour) reduces levels of phosphorylated Akt and phosphorylated MEK. Near-confluent JC cell cultures are serum-starved for 16 hours, then subjected to SKI V pretreatment for 1 hour[2]. SKI V exhibits IC50 values of approximately 2 μM for inhibiting sphingosine kinase (SK) and tumor cell proliferation[1]. SKI V (20 μg/ml) inhibits both purified and endogenous sphingosine kinase (SK) in MDA-MB-231 cells[1]. SKI V (0.2, 1, 5 μM) inhibits the formation of intracellular sphingosine-1-phosphate (S1P) in JC cells in a dose-dependent manner[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.93mL 0.79mL 0.39mL |
19.67mL 3.93mL 1.97mL |
39.33mL 7.87mL 3.93mL |
CAS号 | 24418-86-8 |
分子式 | C15H10O4 |
分子量 | 254.238 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(196.67 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 |