SKI-178 is an in vivo active non-lipid sphingosine kinase 1 (SphK1) inhibitor (IC50 = 0.1-1.8 μM), which induces CDK1-dependent apoptosis in human acute myeloid leukemia cell lines.
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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
99%+ | |||||||||||||||||
Lys05 | ✔ | 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。 |
产品名称 | Potassium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolbutamide | ✔ | 99%+ | |||||||||||||||||
Glimepiride |
++++
SUR2B, IC50: 7.3 nM SUR1, IC50: 5.4 nM |
99%+ | |||||||||||||||||
Dronedarone Hydrochloride | ✔ | 99%+ | |||||||||||||||||
Gliquidone |
++
Potassium channel, IC50: 27.2 nM |
99%+ | |||||||||||||||||
TRAM-34 |
+++
IKCa1 (KCa3.1), Kd: 20 nM |
99%+ | |||||||||||||||||
Glibenclamide | ✔ | 99%+ | |||||||||||||||||
Amiodarone HCl | ✔ | 99%+ | |||||||||||||||||
Gliclazide |
++
Potassium channel, IC50: 184 nM |
99%+ | |||||||||||||||||
Repaglinide | ✔ | 99%+ | |||||||||||||||||
Dofetilide | ✔ | 98% | |||||||||||||||||
Nateglinide | ✔ | 99% | |||||||||||||||||
Quinine hydrochloride dihydrate | ✔ | 99%+ | |||||||||||||||||
ML133 HCl |
+
Kir2.1, IC50: 290 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-178 is a potent inhibitor of sphingosine kinase-1 (SphK1) and SphK2. It exhibits cytotoxicity with IC50 concentrations ranging from 1.8 to 0.1 μM in various cancer cell lines, including those resistant to multiple agents (i.e., MTR3, NCI-ADR, and HL60/VCR cells). SKI-178 induces apoptosis in human acute myeloid leukemia cell lines in a CDK1-dependent manner[1][2]. |
体内研究 | SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) suppresses leukemic progression in the MLL-AF9 model[3]. |
体外研究 | The apoptotic cell death induced by SKI-178 (5 μM; 24 hours) is associated with prolonged phosphorylation of Bcl-2[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.54mL 0.51mL 0.25mL |
12.68mL 2.54mL 1.27mL |
25.35mL 5.07mL 2.54mL |
CAS号 | 1259484-97-3 |
分子式 | C21H22N4O4 |
分子量 | 394.424 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(126.77 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 |