2. Protein Tyrosine Kinase/RTK Autophagy PI3K/Akt/mTOR Epigenetics Apoptosis
  3. FAK ULK AMPK Apoptosis Autophagy
  4. ULK1-IN-2

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).

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ULK1-IN-2 Chemical Structure

ULK1-IN-2 Chemical Structure

CAS No. : 2497409-01-3

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Based on 1 publication(s) in Google Scholar

ULK1-IN-2 Related Antibodies

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Description

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer)[1].

IC50 & Target

ULK1

 

In Vitro

ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7[1].
ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells[1].
ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner[1].
ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.[1].

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

ULK1-IN-2 Related Antibodies

Cell Proliferation Assay

Cell Line: Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7[1]
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.

Cell Autophagy Assay

Cell Line: A549 cells[1]
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24 h
Result: Blocked autophagy of A549 cells via inhibiting ULK.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24 h
Result: Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.
Molecular Weight

495.26

Formula

C19H16BrFN4O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=C(OC)C(OC)=CC(NC2=NC=C(Br)C(OC3=CC=C([N+]([O-])=O)C=C3F)=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (67.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0191 mL 10.0957 mL 20.1914 mL
5 mM 0.4038 mL 2.0191 mL 4.0383 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0191 mL 10.0957 mL 20.1914 mL 50.4785 mL
5 mM 0.4038 mL 2.0191 mL 4.0383 mL 10.0957 mL
10 mM 0.2019 mL 1.0096 mL 2.0191 mL 5.0479 mL
15 mM 0.1346 mL 0.6730 mL 1.3461 mL 3.3652 mL
20 mM 0.1010 mL 0.5048 mL 1.0096 mL 2.5239 mL
25 mM 0.0808 mL 0.4038 mL 0.8077 mL 2.0191 mL
30 mM 0.0673 mL 0.3365 mL 0.6730 mL 1.6826 mL
40 mM 0.0505 mL 0.2524 mL 0.5048 mL 1.2620 mL
50 mM 0.0404 mL 0.2019 mL 0.4038 mL 1.0096 mL
60 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 mL
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ULK1-IN-2 Related Classifications

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-22497409-01-3FAKULKAMPKApoptosisAutophagyPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseUnc-51 like kinaseAMP-activated protein kinaseNon-small cell lung cancer (NSCLC)A549 cellsInhibitorinhibitorinhibit

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