LYN-1604

Catalog No.S8597 Batch:S859701

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Technical Data

Formula

C33H45Cl4N3O2
Molecular Weight 657.54 CAS No. 2088939-99-3
Solubility (25°C)* In vitro Water 100 mg/mL (152.08 mM)
Ethanol 100 mg/mL (152.08 mM)
DMSO 50 mg/mL (76.04 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.78mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.7mg/ml Taking the 1 mL working solution as an example, add 50 μL of 94 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Targets
ULK1 [1]
18.94 nM(EC50)
In vitro LYN-1604 is a ULK1 agonist. Three amino acid residues (LYS50, LEU53, and TYR89) are key to the activation site of LYN-1604 and ULK1 by site-directed mutagenesis and biochemical assays. LYN-1604 induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 is bound to wild-type ULK1 with a binding affinity in the nanomole range (KD = 291.4 nM), but the ULK1Y89A mutant protein causes a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1K50A and ULK1L53A mutants[1].
In vivo LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. LYN-1604 can directly activate ULK1, the initiator of autophagy, thereby inducing cell death to inhibit the growth of triple negative breast cancer (TNBC) in vitro and in vivo[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MDA-MB-231 cells

  • Concentrations

    0.5, 1.0 and 2.0 μM

  • Incubation Time

    24 h

  • Method

    Cells are dispensed in 96-well plates at a density of 5 × 104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of compounds for the indicated time periods. Cell viability is measured by the MTT assay.
Animal Study:

[1]
  • Animal Models

    MDA-MB-231 xenograft model (BALB/c nude mice)

  • Dosages

    25 mg/kg, 50 mg/kg, 100 mg/kg

  • Administration

    intragastric administration

Selleck's LYN-1604 has been cited by 3 publications

Piceatannol enhances Beclin-1 activity to suppress tumor progression and its combination therapy strategy with everolimus in gastric cancer [ Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9] PubMed: 36271983
Synergetic contributions of viral VP1, VP3, and 3C to activation of the AKT-AMPK-MAPK-MTOR signaling pathway for Seneca Valley virus-induced autophagy [ J Virol, 2021, JVI0155021] PubMed: 34757844
Corneal autophagy and ocular surface inflammation: A new perspective in dry eye. [ Exp Eye Res, 2019, 184:126-134] PubMed: 31018117

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.