2. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Lipoxygenase Apoptosis Reactive Oxygen Species (ROS) FAK
  4. LXG6403

LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors.

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LXG6403 Chemical Structure

LXG6403 Chemical Structure

CAS No. : 315705-04-5

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LXG6403 Related Antibodies

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Description

LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors[1].

In Vitro

LXG6403 (Compound 9) inhibits the cellular LOX activity with IC50s of 1.3 μM (MDA-MB-231 cells), 1.43 μM (HCC143 cells), 4.14 μM (Hs-578-T cells), and 3.0 μM (HCC1937 cellss)[1].

LXG6403 (0-10 μM) inhibits rLOX, rLOXL2, rLOX-CM, rLOXL2-CM activity ,with IC50s of 0.28 μM, 0.95 μM, 0.95 μM, 2.82 μM respectively, does not inhibit rLOXL1 (IC50 > 10 μM) in HEK293T cells[1].

LXG6403 (0-20 μM) inhibits pronase-mediated degradation of LOX[1].

LXG6403 (15 μM, 48 h) enhances response to the anthracycline, Doxorubicin (HY-15142A); the platinum-based agent, Cisplatin (HY-17394); and the taxane, Paclitaxel (HY-B0015) in the TNBC cells, MDA-MB-231, and HCC1143 in 3D collagen I[1].

LXG6403 (9 days) reduces organoid viability and size with chemotherapeutic agents; Doxorubicin, Cisplatin, or Paclitaxel[1].

LXG6403 (20 µM, 48 h) inhibits the migration capacity of the highly migratory MDA-MB-231 cells[1].

LXG6403 (15 μM) reduces deposition of collagen and fibronectin within the ECM and inhibited their assembly[1].

LXG6403 improves Doxorubicin penetration in 3D collagen I-embedded TNBC cell lines and PDX organoids[1].

LXG6403 inhibits LOX, increases drug penetration in 3D culture, induces ROS generation/DNA damage and inhibits FAK signaling, leading to G1 arrest and apoptosis in TNBC cell lines and organoids in MDA-MB-231 cells[1].

LXG6403 (2.5-20 μM) not change cell viability in MCF12A, HUVEC, and HFF-1 cells[1].

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

LXG6403 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 20 μM
Incubation Time: 24 h, 48 h
Result: Increased ɣ-H2AX levels, cleaved caspase-3 and cleaved PARP levels, and decreased FAK phosphorylation.
In Vivo

LXG6403 (Compound 9) (25-200 mg/kg, p.o., 5 days) does not change body weight or blood cell counts and does not cause organ damage in BALB/c mice[1].

LXG6403 (50 mg/kg, P.O., daily, 24 days) reduces fibrillar collagen content/crosslinking, leading to increased drug penetration and ROS accumulation, inhibits FAK signaling, induces DNA damage, G1 arrest, and apoptosis combined with Doxorubicin treatment in the resistant TM01278 TNBC PDX mice model with high LOX expression[1].

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

Animal Model: TM01278 TNBC PDX mice model[1]
Dosage: 50 mg/kg
Administration: P.O., daily, 24 days
Result: Reduced tumor growth and tumor weight without changing body weight combined with Doxorubicin.
Reduced fibrillar collagen and insoluble collagen content combined with Doxorubicin.
Increased doxorubicin penetration in vivo, increased ROS accumulation (and DNA damage, further leading to FAK inhibition, induction of G1 arrest and apoptosis combined with Doxorubicin.
Molecular Weight

345.44

Formula

C15H15N5OS2
CAS No.
SMILES

O=C(C)NC1=CC=C(NC2=NC(C3=C(C)N=C(N)S3)=CS2)C=C1
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References
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LXG6403 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:

LXG6403315705-04-5LXG 6403LXG-6403LipoxygenaseApoptosisReactive Oxygen Species (ROS)FAKLOXPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorMDA-MB-231 cellsHEK293T mammalian cellsTM01278 TNBC PDX modelinhibitorinhibit

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