SML1540
SBI-0206965
≥98% (HPLC), serine/threonine autophagy-initiating kinases ULK1 and ULK2 inhibitor, powder
别名:
2-（（5-溴-2-（（3,4,5-三甲氧基苯基）氨基）嘧啶-4-基）氧）-N-甲基苯甲酰胺
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关于此项目
经验公式（希尔记法）:
C21H21BrN4O5
化学文摘社编号:
分子量:
489.32
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
产品名称
SBI-0206965, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
SMILES string
BrC1=C(OC2=C(C(NC)=O)C=CC=C2)N=C(NC3=CC(OC)=C(OC)C(OC)=C3)N=C1
InChI
1S/C21H21BrN4O5/c1-23-19(27)13-7-5-6-8-15(13)31-20-14(22)11-24-21(26-20)25-12-9-16(28-2)18(30-4)17(10-12)29-3/h5-11H,1-4H3,(H,23,27)(H,24,25,26)
InChI key
NEXGBSJERNQRSV-UHFFFAOYSA-N
Application
SBI-0206965已用于研究其对镉转化的前列腺上皮细胞生长的影响。
Biochem/physiol Actions
由于大多数肿瘤细胞通过自噬机制存活，因此抑制自噬诱导物Unc-51（丝氨酸/苏氨酸蛋白激酶）样自噬激活激酶（ULK1和ULK2）可能在癌症治疗中有用。
SBI-0206965 是丝氨酸/苏氨酸自噬起始激酶 ULK1 和 ULK2 的强效选择性抑制剂，对 ULK1 具有选择性。
SBI-0206965 是丝氨酸/苏氨酸自噬起始激酶 ULK1 和 ULK2 的强效选择性抑制剂，对 ULK1 具有选择性。 SBI-0206965对于ULK1的IC50值为108 nM，而对于ULK2为711 nM。 肿瘤细胞需要自噬来清除错误折叠的蛋白质或受损的细胞器。SBI-0206965可抑制mTOR抑制诱导的细胞自噬。 mTOR信号通常在许多肿瘤中过度活跃，并能驱动增殖，所以mTOR抑制剂作为抗癌药物正在被研究。 然而，mTOR抑制也会导致激活依赖于ulk1的自噬生存反应，而mTOR抑制剂的大多数结果最多只能起到细胞抑制作用。 SBI-0206965协同mTOR抑制诱导细胞凋亡和死亡。
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Structure and function of the ULK1 complex in autophagy.
Lin M G and James H H
Current Opinion in Cell Biology, 39, 61-68 (2016)
Venkatesh Kolluru et al.
Cancer letters, 408, 121-129 (2017-08-29)
Chronic exposure to cadmium is known to be a risk factor for human prostate cancer. Despite over-whelming evidence of cadmium causing carcinogenicity in humans, the specific underlying molecular mechanisms that govern metal-induced cellular transformation remain unclear. Acute exposure (up to
Séverine Olivier et al.
International journal of molecular sciences, 20(20) (2019-10-23)
The AMP-activated protein kinase (AMPK) is principally known as a major regulator of cellular energy status, but it has been recently shown to play a key structural role in cell-cell junctions. The aim of this study was to evaluate the
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML1540-5MG | 04061832452081 |
| SML1540-25MG | 04061832452074 |