2. Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein TGF-beta/Smad Apoptosis
  3. Farnesyl Transferase Ras TGF-β Receptor Apoptosis
  4. L-744832

L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.

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L-744832

L-744832 Chemical Structure

CAS No. : 160141-09-3

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L-744832 Related Antibodies

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K-Ras H-Ras N-Ras Ras

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

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Description

L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer[1][2].

In Vitro

L-744832 (0.1-50 μM, 24-72 h) shows significant differences in sensitivity in Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells with IC50s of 1.3, 2.1, 12.3, 14.3 and > 50 μM[1].
L-744832 (0.1-50 μM, 72 h) arrest the sensitive cell lines (Panc-1, Capan-2, BxPC-3 and AsPC-1) in the G2/M phase of the cell cycle and the arrest occurs during the mitotic entry stage downstream of the G2/M checkpoint[1].
L-744832 (10 μM, 24-72 h) induces above five types of cell apoptosis, and the combination of radiotherapy can significantly increase the apoptosis rate of MIA PaCa-2 cells, while this effect is not observed in BxPC-3 cells[1][2].
L-744832 (0.1-10 μM) with ionizing radiation results in enhanced cytotoxicity in human pancreatic cancer cells[1].
L-744832 (5-10 μM) effectively inhibits the farnesylation of H-Ras and N-Ras and MIA PaCa-2 cells are more sensitive than BxPC-3 cells[2].
L-744832 (5-10 μM, 3-6 h) restores the expression of TGF-β type II receptor (RII) through regulating DNMT1, thereby re-establishing the tumor-suppressing function of TGF-β[2].

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

L-744832 Related Antibodies

Cell Cycle Analysis[2]

Cell Line: Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
Concentration: 0.1, 0.5, 1, 10, 25 and 50 μM
Incubation Time: 72 h
Result: Dose-dependent increased in G2/M phase accumulation and the proportion of G2/M phase cells in Panc-1 cells increased nearly threefold.

Apoptosis Analysis[2]

Cell Line: Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Showed chromatin condensation and nuclear fragmentation.
Increased the apoptotic index in each group, and this occurred in both wild-type p53 (Capan-2) cells and mutant p53 (Panc-1) cells.

Western Blot Analysis[2]

Cell Line: Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Significantly increased the activity of Cyclin B1/Cdc2 kinase.

RT-PCR[1]

Cell Line: MIA PaCa-2 cells
Concentration: 10 μM
Incubation Time: 3 and 6 h
Result: Activated the RII promoter to increase its mRNA levels.
Reduced the mRNA levels of DNMT1.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 10 μM
Incubation Time: 3 and 6 h
Result: Activated the RII promoter to increase its protein levels.
Reduced the protein levels of DNMT1.
Molecular Weight

559.78

Formula

C26H45N3O6S2
CAS No.
SMILES

O=C(OC(C)C)[C@@H](NC([C@@H](OC[C@@H](NC[C@@H](N)CS)[C@@H](C)CC)CC1=CC=CC=C1)=O)CCS(=O)(C)=O
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L-744832 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.

Keywords:

L-744832160141-09-3L744832L 744832Farnesyl TransferaseRasTGF-β ReceptorApoptosisFtaseTransforming growth factor beta receptorspancreatic cancerTGF-b signalingradio-sensitizationfarnesyltransferase inhibitor (FTI)DNA methyltransferaseTGF-b type II receptor (TGF-bRII)Inhibitorinhibitorinhibit

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