ABC294640 markedly alters the ratio of ceramide/S1P consistent with inhibition of SK activity in MDA-MB-231 cells.
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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。 |
描述 | Sphingosine is an intermediate of sphingolipids that can be rapidly phosphorylated by sphingosine kinase (SK1 and SK2) to produce sphingosine 1-phosphate, which is a mitogenic compound. ABC294640 is a selective inhibitor of SK2 with a Ki value of 9.8 μM. ABC294640 dose-dependently inhibited recombinant human SK2 with an IC50 value of 60μM, while the activity of SK1 was not affected by ABC294640 at the concentration up to 100μM. In MDA-MB-231 cells, ABC294640 decreased [3H]S1P formation in a dose-dependent manner with an IC50 value of 26μM. ABC294640 also inhibited the proliferation of human tumor cell lines (1025LU, A-498, Caco-2, HT-29, DU145, SK-OV-3) with IC50 values ranging from 10.5-48.1μM[2]. In a mouse model of tri-nitrobenzene sulfonic acid (TNBS)-induced colitis, oral administration of ABC294640 (50mg/kg, twice daily) decreased TNBS-induced increase in mucosal myeloperoxidase activity by 60%. The histological analysis on colon sections revealed that the inflammation and damage caused by TNBS was reduced or negated by ABC294640 treatment[3]. |
Dose | Mice[2] (p.o.): min = 50 mg/kg, max = 100 mg/kg |
Administration | p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.13mL 2.63mL 1.31mL |
26.25mL 5.25mL 2.63mL |
CAS号 | 915385-81-8 |
分子式 | C23H25ClN2O |
分子量 | 380.91 |
别名 | Opaganib |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 | |
动物实验配方 |
2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL |