1. Autophagy
  2. ULK

LYN-1604 hydrochloride 

Cat. No.: HY-101923A Purity: 99.80%
Data Sheet SDS Handling Instructions

LYN-1604 hydrochloride is a potent ULK1 agonist with an EC50 of 18.94 nM.

For research use only. We do not sell to patients.
LYN-1604 hydrochloride Chemical Structure

LYN-1604 hydrochloride Chemical Structure

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10 mM * 1 mL in DMSO USD 197 In-stock
5 mg USD 144 In-stock
10 mg USD 252 In-stock
25 mg USD 528 In-stock
50 mg USD 864 In-stock
100 mg USD 1500 In-stock
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Description

LYN-1604 hydrochloride is a potent ULK1 agonist with an EC50 of 18.94 nM.

IC50 & Target

EC50: 18.94 nM (ULK1)[1]

In Vitro

LYN-1604 is found as a potential ULK1 agonist with enzymatic activity of 195.7% at 100 nM and IC50 of 1.66 μM against MDA-MB-231 cells. LYN-1604 displays a good effect on ULK1 activation with an EC50 of 18.94 nM. LYS50, LEU53, and TYR89 are key to the activation site of LYN-1604. LYN-1604 induces cell death in MDA-MB-231 cells. LYN-1604 could modulate ATF3 and RAD21 through ULK1 in MDA-MB-231 cells. LYN-1604 can also increase cleavage of caspase3 and induce apoptosis. LYN-1604 induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis[1].

In Vivo

LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. The body weights of mice are stable. LYN-1604 induces remarkable autophagy in vivo. LYN-1604 has good therapeutic potential by targeting ULK1-modulated cell death of TNBC, thus making a ULK1 agonist that can be utilized as a new drug for triple negative breast cancer therapy[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.6101 mL 8.0505 mL 16.1010 mL
5 mM 0.3220 mL 1.6101 mL 3.2202 mL
10 mM 0.1610 mL 0.8050 mL 1.6101 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

The ULK1 kinase enzyme, substrate, ATP and compound (include LYN-1604) are diluted in kinase buffer. Then, 1 μL of compound or (5% DMSO), 2 μL of ULK1 kinase enzyme or purified wild-type and mutant ULK1 (K50A, L53A, Y89A) (10 ng), or 2 μL of MBP (0.1 μg/μL)/ATP (10 μM) mix are added to the wells of a 384 well low volume plate. After incubation at room temperature for 60 minutes, 5 μL of kinase assay reagent is added per well. The plates are incubated at room temperature for 40 minutes and then 10 μL of kinase detection reagent is added. After incubation at room temperature for 30 minutes, the luminescence is recorded. The EC50 values are calculated using nonlinear regression with normalized dose response fitting[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

MCE-7, MDA-MB-231 and MDA-MB-468 cells are treated with LYN-1604, cell viability is measured by the MTT assay[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Mice are injected subcutaneously with MDA-MB-231 cells. When the tumors reach 100 mm3 in volume, the mice are divided into four groups. Three groups are treated with different doses of LYN-1604 once a day by intragastric administration for 14 days (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg), whereas the control group is treated with vehicle control. During the treatment, the tumor volumes and body weight are measured every day until the end of the study. At the end of treatment, all mice are sacrificed. The spleen, liver, kidney and tumor tissue are harvested, weighed, and photographed, then immediately frozen in liquid nitrogen or fixed in formalin[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

621.08

Formula

C₃₃H₄₄Cl₃N₃O₂

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥100 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.80%

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LYN-1604 hydrochloride
Cat. No.:
HY-101923A
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