2. Autophagy
  3. ULK
  4. ULK1-IN-4

ULK1-IN-4 (compound 12i) 是一种 ULK1 抑制剂，其对人源 ULK1 的 IC50 为 4.7 μM，且对 Aurora A/Aurora B 激酶具有选择性。ULK1-IN-4 可与 ULK1 的 Cys182 残基的巯基形成共价键，从而抑制 ULK1 的激酶活性。ULK1-IN-4 可抑制结直肠癌细胞的生长，且在结直肠癌小鼠模型中表现出肿瘤抑制活性。

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ULK1-IN-4

ULK1-IN-4 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ULK1-IN-4 (compound 12i) is a ULK1 inhibitor with an IC50 of 4.7 μM against human ULK1, and it exhibits selectivity for Aurora A/Aurora B kinases. ULK1-IN-4 forms a covalent bond with the thiol group of the Cys182 residue of ULK1, thereby inhibiting the kinase activity of ULK1. ULK1-IN-4 inhibits the growth of colorectal cancer cells and exerts tumor-suppressive activity in a mouse model of colorectal cancer[1].

体外研究
(In Vitro)

ULK1-IN-4 (compound 12i) (concentrations used to determine IC50; 60 min) 可在体外强效抑制 ULK1 激酶活性，其 IC50 为 4.7 μM；同时该化合物还可抑制 ULK2，且对 Aurora A/Aurora B 激酶具有高选择性[1]。
ULK1-IN-4 (1-100 μM; 60 s association, 120 s dissociation) 可通过 BLI 结合动力学实验证明[1]，与 ULK1 激酶形成不可逆的共价键。
ULK1-IN-4 (200 μM; 24 h) 可共价结合人源 ULK1 激酶的 Cys182 残基[1]。
ULK1-IN-4 (gradient concentrations used to determine IC50; 48 h) 可抑制 SW620、HCT116 的增殖，其 IC50 值分别为 13.31 μM、9.76 μM[1]。
ULK1-IN-4 (5-10 μM; 2 weeks) 以剂量依赖的方式抑制 SW620、HCT116 和 CT26 结直肠癌细胞 (CRC 细胞) 的长期集落形成[1]。
ULK1-IN-4 (10-20 μM; 48 h) 可在处理 48 h 后诱导 SW620、HCT116 和 CT26 结直肠癌 (CRC) 细胞发生 S 期或 G2/M 期细胞周期阻滞[1]。
ULK1-IN-4 (2.5-10 μM; 48 h) 可在处理 48 h 后抑制 SW620、HCT116 和 CT26 结直肠癌细胞 (CRC cells) 中的自噬，这一点可通过自噬相关蛋白的表达变化得到证实[1]。
ULK1-IN-4 (2.5-10 μM; 48 h) 可在处理 48 h 后激活 SW620、HCT116 和 CT26 结直肠癌细胞 (CRC 细胞) 的凋亡通路，这一点可通过凋亡相关蛋白的表达变化得到证实[1]。
ULK1-IN-4 (10 μM; 24 h) 可在基础自噬和雷帕霉素诱导的自噬条件下，抑制 HCT116 结直肠癌细胞经 24 h 处理后的早期自噬流[1]。
ULK1-IN-4 (10-20 μM; 48 h) 以剂量依赖的方式在处理 48 h 后诱导 SW620、HCT116 和 CT26 结直肠癌 (CRC) 细胞发生凋亡[1]。
ULK1-IN-4 (5-10 μM; 24-48 h) 以剂量依赖的方式抑制 SW620、HCT116 和 CT26 结直肠癌细胞 (CRC 细胞) 的迁移能力，处理时间为 24 h 和 48 h[1]。
ULK1-IN-4 (5-10 μM; 24 h) 可在处理 24 h 后抑制 SW620、HCT116 和 CT26 结直肠癌 (CRC) 细胞的迁移能力，并上调 E-cadherin 的表达[1]。
ULK1-IN-4 (10 μM; 48 h) 可发挥多种药理学作用，包括细胞周期阻滞、迁移抑制、自噬抑制和凋亡诱导，这些作用在 SW620 结直肠癌细胞中依赖于对 ULK1 的靶向作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ULK1-IN-4 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: Gradient concentrations used to determine IC50
Incubation Time: 48 h
Result: Inhibited proliferation of SW620 cells with an IC50 of 13.31 μM.
Inhibited proliferation of HCT116 cells with an IC50 of 9.76 μM.
Inhibited proliferation of CT26 cells with an IC50 of 13.07 μM.

Cell Proliferation Assay[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: 5-10 μM
Incubation Time: 2 weeks (continuous treatment)
Result: Dose-dependently reduced both the number and size of colonies in SW620, HCT116, and CT26 cells.

Cell Cycle Analysis[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: 10-20 μM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the S or G2/M phase in all three cell lines: in SW620 cells, 10 μM caused G1:63.2%, S:19.27%, G2/M:16.96%; 20 μM caused G1:58.9%, S:23.3%, G2/M:17.5%.
In HCT116 cells, 10 μM caused G1:88.65%, S:11.38%, G2/M:9.22%; 20 μM caused G1:88.61%, S:16.88%, G2/M:14.12%.
In CT26 cells, 10 μM caused G1:59.27%, S:24.35%, G2/M:16.25%; 20 μM caused G1:55.48%, S:24.34%, G2/M:19.55%.

Western Blot Analysis[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: 2.5-10 μM
Incubation Time: 48 h
Result: Dose-dependently increased levels of the autophagy substrate p62.
Reduced conversion of LC3 I to LC3 II.
Decreased levels of Beclin1 and phospho-Beclin-1 (Ser15) in all three cell lines.\nDose-dependently upregulated expression levels of cleaved-caspase-3 and cleaved-PARP.
Increased levels of the pro-apoptotic protein Bax.
Downregulated levels of the anti-apoptotic protein Bcl2 in all three cell lines.

Apoptosis Analysis[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: 10-20 μM
Incubation Time: 48 h
Result: Dose-dependently increased the proportion of apoptotic cells (early + late) in all three cell lines: in SW620 cells, 10 μM caused 26.01% apoptosis, 20 μM caused 63.79% apoptosis; in HCT116 cells, 10 μM caused 19.52% apoptosis, 20 μM caused 45.18% apoptosis; in CT26 cells, 10 μM caused 12.81% apoptosis, 20 μM caused 100.68% apoptosis.

Cell Migration Assay[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: 5-10 μM
Incubation Time: 24 h; 48 h
Result: Dose-dependently suppressed wound closure in all three cell lines after 24 and 48 h of treatment.

Cell Migration Assay[1]

Cell Line: Human colorectal cancer cell lines SW620, HCT116; mouse colorectal cancer cell line CT26
Concentration: 5-10 μM
Incubation Time: 24 h
Result: Dose-dependently reduced the number of migrated cells in all three cell lines.
Upregulated levels of E-cadherin.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-∞ CL Vz Tmax Cmax Bioavailability
Rat[1] 10 mg/kg i.v. 2.94 h 467.26 ng·h/mL 1446.71 mL/min/kg 725.27 L/kg 0.25 h / /
Rat[1] 10 mg/kg p.o. 5.66 h 185.42 ng·h/mL 951.78 mL/min/kg 496.76 L/kg 2 h 21.67 ng/mL 39.7 %
体内研究
(In Vivo)

ULK1-IN-4 (20-40 mg/kg; i.p.; once every two days; 14 days) 可在体内以剂量依赖方式抑制 Balb/c 小鼠的结直肠肿瘤生长，在 40 mg/kg 剂量下的肿瘤生长抑制率达 70.4%，且未观察到全身毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c (6-7-week-old female, subcutaneously injected with 1×106 CT26 cells)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; once every two days; 14 days
Result: Achieved a tumor growth inhibition (TGI) rate of 19.2% and an average tumor weight of 0.873 g at 20 mg/kg.
Achieved a TGI rate of 70.4% and an average tumor weight of 0.327 g at 40 mg/kg.
Caused no significant body weight loss or abnormal behaviors during treatment.
Showed no significant histopathological changes in heart, liver, spleen, lungs, and kidneys compared to controls.
Downregulated ULK1, p-Beclin-1 (Ser15), and Beclin-1 expression, upregulated p62 expression, increased TUNEL-positive apoptotic cells, elevated cleaved-caspase 3 levels, and reduced Ki67-positive proliferative cells at 40 mg/kg.
分子量

533.02

Formula

C29H29ClN4O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ULK1-IN-4 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ULK1-IN-4ULKUnc-51 like kinaseautophagic fluxCys182Balb/c miceAurora B kinasesapoptosisULK2ULK1colorectal carcinoma cellsAurora A kinasescell cycle arrestInhibitorinhibitorinhibit

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