1. Cell Cycle/DNA Damage
    Cytoskeleton
    Apoptosis
  2. PAK
    Apoptosis
  3. LCH-7749944

LCH-7749944 (Synonyms: GNF-PF-2356)

Cat. No.: HY-125035 Purity: 99.43%
Handling Instructions

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.

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

LCH-7749944 Chemical Structure

LCH-7749944 Chemical Structure

CAS No. : 796888-12-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].

IC50 & Target[1]

PAK4

14.93 μM (IC50)

In Vitro

LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner[1].
LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells[1].
LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase[1].
LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells
Concentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.

Apoptosis Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20 μM
Incubation Time: 12, 24, 48 hours
Result: Induced apoptosis of SGC7901 cells.

Cell Cycle Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20 μM
Incubation Time: 12, 24, 48 hours
Result: Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.

Western Blot Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20, 30 μM
Incubation Time: 24 hours
Result: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.
Molecular Weight

350.41

Formula

C₂₀H₂₂N₄O₂

CAS No.

796888-12-5

SMILES

COC1=CC(NC2=NC(NCC3OCCC3)=C4C=CC=CC4=N2)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (713.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8538 mL 14.2690 mL 28.5380 mL
5 mM 0.5708 mL 2.8538 mL 5.7076 mL
10 mM 0.2854 mL 1.4269 mL 2.8538 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LCH-7749944GNF-PF-2356LCH7749944LCH 7749944PAKApoptosisp21 activated kinasesproliferationhumangastriccancercellsPAK4c-SrcEGFRcyclinD1Inhibitorinhibitorinhibit

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Product Name:
LCH-7749944
Cat. No.:
HY-125035
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