SBI-0206965是一种高效、选择性、细胞渗透性 ULK1 激酶抑制剂,对 ULK1 激酶的 IC50 为 108 nM,对密切相关的激酶 ULK2 的 IC50 为 711 nM。
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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 |
97% | |||||||||||||||||
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。 |
靶点 |
|
描述 | SBI-0206965 is identified as a potent and selective inhibitor of the autophagy kinase ULK1, showing cell permeability with an IC50 of 108 nM for ULK1 kinase. It also exhibits inhibition towards ULK2, although with lesser potency, having an IC50 of 711 nM[1]. |
体内研究 | In vivo, a dose of 50 mg/kg of SBI-0206965, administered intraperitoneally once every three days for a duration of 37 days, effectively inhibits tumor growth and promotes apoptosis in A498 xenograft tumors, showcasing its therapeutic potential in cancer treatment[1]. |
体外研究 | When administered at concentrations ranging from 5 to 20 μM for 24 hours, SBI-0206965 triggers apoptosis in A498 and ACHN cells under starvation conditions. This apoptotic induction is further evidenced by the attenuation of Ser108 phosphorylation on the AMPK β1 subunit alongside increased levels of cleaved Caspase 8 and PARP, which are established markers of apoptosis[1]. |
作用机制 | SBI-0206965 occupies a pocket that partially overlaps the ATP active site in a type Iib inhibitor manner. |
Dose | Mice: 5 mg/kg - 20 mg/kg[2] (i.p.), 50 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.22mL 2.04mL 1.02mL |
20.44mL 4.09mL 2.04mL |
CAS号 | 1884220-36-3 |
分子式 | C21H21BrN4O5 |
分子量 | 489.319 |
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 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(214.58 mM),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 |