ULK-101

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Chemical Structure| 2443816-45-1 同义名 : -
CAS号 : 2443816-45-1
货号 : A1149867
分子式 : C22H16F4N4OS
纯度 : 99%+
分子量 : 460.45
MDL号 : MFCD31813791
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(184.6 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：
生物活性
描述 Nnc-51 like autophagy initiating kinase 1 (ULK1) is a serine/threonine kinase that works as a part of a complex with binding partners ATG13, RB1CC1, and ATG101 in autophagy induction. ULK-101 is a potent, selective inhibitor of ULK1 with an IC50 value of 8.3 nM in vitro, whereas the inhibitory effect of ULK-101 on ULK2 is weaker with an IC50 value of 30 nM. In 293FT cells expressing ULK1, ULK-101 at the doses of 60 – 1000 nM dose-dependently inhibited Ser15 phosphorylation with an EC50 value of 390 nM. In U2OS cells stably expressing omegasome marker, EGFP-DFCP1, 2.5-h treatment with 5 μM ULK-101 completely inhibited the formation of DFCP1-positive structures induced by AZD8055 (100 nM). ULK-101 at the same dose also strongly reduced AZD8055-induced phagophore formation. Incubation of U2OS cells with ULK-101 (300 – 5000 nM) for 3 hours reduced BafA1-induced LC3B-II accumulation in a concentration-dependent manner with an EC50 value of 700 nM. Also, ULK-101 treatment led to a 6-fold reduction of BafA1-induced accumulation of LC3B-positive vesicles as compared to the vehicle control. ULK-101 reduced cell viability of U2OS cells when they were cultured in both Optistarve (OS) and full growth media (FM) with EC50 values of 6.3 and 22.3 μM, respectively. Furthermore, KRAS mutant or amplified non-small-cell lung cancer cell lines demonstrated a 5-fold increase in ULK-101 sensitivity when cultured in OS compared with FM[1].
作用机制 ULK-101 is a ULK1 inhibitor. It blocks the autophagy induction and suppresses autophagic flux in response to multiple stimuli.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.86mL

2.17mL

1.09mL

21.72mL

4.34mL

2.17mL
参考文献

[1]Martin KR, Celano SL, Solitro AR, Gunaydin H, Scott M, O'Hagan RC, Shumway SD, Fuller P, MacKeigan JP. A Potent and Selective ULK1 Inhibitor Suppresses Autophagy and Sensitizes Cancer Cells to Nutrient Stress. iScience. 2018 Oct 26;8:74-84. doi: 10.1016/j.isci.2018.09.012. Epub 2018 Sep 19. PMID: 30292171; PMCID: PMC6172447.