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

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.

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ULK1-IN-4

ULK1-IN-4 Chemical Structure

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Description

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].

In Vitro

ULK1-IN-4 (compound 12i) (5-10 μM; 24-48 h) inhibits the migratory capacity of SW620, HCT116, and CT26 CRC cells in a dose-dependent manner after 24 and 48 h of treatment[1].
ULK1-IN-4 (5-10 μM; 24 h) inhibits the migratory capacity of SW620, HCT116, and CT26 CRC cells after 24 h of treatment, and increases E-cadherin expression[1].
ULK1-IN-4 (10 μM; 48 h) exerts pharmacological effects, including cell cycle arrest, migration inhibition, autophagy suppression, and apoptosis induction, that are dependent on ULK1 targeting in SW620 CRC cells[1].

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

ULK1-IN-4 Related Antibodies

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.
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 %
In Vivo

ULK1-IN-4 (20-40 mg/kg; i.p.; once every two days; 14 days) inhibits colorectal tumor growth in Balb/c mice in vivo in a dose-dependent manner, achieving a 70.4% tumor growth inhibition rate at the 40 mg/kg dose, with no observed systemic toxicity[1].

MedChemExpress (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.
Molecular Weight

533.02

Formula

C29H29ClN4O4
SMILES

COC(C=C1)=CC=C1N/C(C2=CC=CC=C2)=C3C(C=C(NC(CCCCNC(CCl)=O)=O)C=C4)=C4NC/3=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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ULK1-IN-4 Related Classifications

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Help & FAQs
  • 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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