1. Autophagy Apoptosis
  2. ULK Autophagy Apoptosis
  3. LYN-1604

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (LYN-1604 dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

LYN-1604 Chemical Structure

LYN-1604 Chemical Structure

CAS No. : 2088939-99-3

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Description

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC)[1].

IC50 & Target[1]

ULK1

18.94 nM (EC50)

In Vitro

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) [1].
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) [1].
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells[1].
LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells[1].
LYN-1604 induces ATG5-dependent autophagy via the ULK complex[1].
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis[1].

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

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1.0 and 2.0 μM
Incubation Time:
Result: Induced cell death. Autophagy ratio was increased in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, and 2 μM
Incubation Time: 24 hours
Result: Induced remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II.
In Vivo

LYN-1604 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg; intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death[1].

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

Animal Model: 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g)[1]
Dosage: Low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg
Administration: Intragastric administration; once a day for 14 days
Result: Significantly inhibited the growth of xenograft MDA-MB-231 cells. The body weights of mice were stable. By the end of the experiment, the liver and spleen weight indexes of mice were slightly increased in parts of the groups, while the kidney weight index was not affected in all dose groups.
Molecular Weight

584.62

Formula

C33H43Cl2N3O2

CAS No.
SMILES

ClC1=CC=C(C(CN2CCN(C(CN(CC(C)C)CC(C)C)=O)CC2)OCC3=CC=C(C=CC=C4)C4=C3)C(Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (171.05 mM; Need ultrasonic and warming; 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 1.7105 mL 8.5526 mL 17.1051 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7105 mL 8.5526 mL 17.1051 mL 42.7628 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL 8.5526 mL
10 mM 0.1711 mL 0.8553 mL 1.7105 mL 4.2763 mL
15 mM 0.1140 mL 0.5702 mL 1.1403 mL 2.8509 mL
20 mM 0.0855 mL 0.4276 mL 0.8553 mL 2.1381 mL
25 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7105 mL
30 mM 0.0570 mL 0.2851 mL 0.5702 mL 1.4254 mL
40 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0691 mL
50 mM 0.0342 mL 0.1711 mL 0.3421 mL 0.8553 mL
60 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
80 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5345 mL
100 mM 0.0171 mL 0.0855 mL 0.1711 mL 0.4276 mL
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LYN-1604 Related Classifications

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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.

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Product Name:
LYN-1604
Cat. No.:
HY-101923
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