1. Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. Src Interleukin Related
  3. LDDN-0003499

LDDN-0003499 is a Src family tyrosine kinase inhibitor and anti-inflammatory agent. LDDN-0003499 reduces basal and Aβ-stimulated levels of active, phosphorylated Lyn and Src kinases, and attenuates Aβ-stimulated secretion of pro-inflammatory cytokines TNFα and IL-6 in microglial cells. LDDN-0003499 can be used for the research of Alzheimer's disease.

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

LDDN-0003499

LDDN-0003499 Chemical Structure

CAS No. : 331662-51-2

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Description

LDDN-0003499 is a Src family tyrosine kinase inhibitor and anti-inflammatory agent. LDDN-0003499 reduces basal and Aβ-stimulated levels of active, phosphorylated Lyn and Src kinases, and attenuates Aβ-stimulated secretion of pro-inflammatory cytokines TNFα and IL-6 in microglial cells. LDDN-0003499 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

IL-6

 

In Vitro

LDDN-0003499 (0.5 nM-50 μM; 24 h) shows no toxicity to mouse microglial BV2 cells[1].
LDDN-0003499 (0.5 nM-50 μM; 1 h) reduces the total protein phosphotyrosine level in murine microglial BV2 cells in a dose-dependent manner[1].
LDDN-0003499 (0.5 nM-50 μM; 1 h) dose-dependently inhibits the basal activity levels of phosphorylated Lyn and Src in mouse microglial BV2 cells[1].
LDDN-0003499 (0.5 nM-50 μM; 65 min) dose-dependently inhibits the Aβ-induced increase in the levels of activated phosphorylated Lyn and Src in mouse microglial BV2 cells[1].
LDDN-0003499 (0.5 nM-50 μM; 1 h) reduces Aβ-stimulated secretion of TNF-α and IL-6 in mouse microglial BV2 cells in a dose-dependent manner[1].
LDDN-0003499 (1 μM) exhibits moderately high NADPH-dependent clearance and low non-NADPH-dependent clearance in human and mouse liver microsomes[1].

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

Western Blot Analysis[1]

Cell Line: unstimulated murine microglial BV2 cells
Concentration: 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM, 50 μM
Incubation Time: 1 h
Result: Produced a dose-dependent decrease in active, phosphorylated Lyn (pLyn) and Src (pSrc) protein levels.
Did not alter phosphorylated levels of ERK, JNK, or p38.

Western Blot Analysis[1]

Cell Line: Aβ-stimulated murine microglial BV2 cells
Concentration: 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM, 50 μM
Incubation Time: 1 h (pre-incubation); 5 min (co-incubation with 1 μM Aβ1-42)
Result: Attenuated the Aβ-stimulated increase in active, phosphorylated Lyn and Src protein levels.
Significantly attenuated the Aβ-stimulated increase in pLyn at 50 nM, while 500 nM was required for pSrc, demonstrating 10-fold selectivity for Lyn over Src in this paradigm.
Did not inhibit Aβ-stimulated increases in phosphorylated ERK.
Molecular Weight

350.20

Formula

C16H13Cl2N3O2

CAS No.
SMILES

ClC1=CC=C(NC=2N=CN=C3C=C(OC)C(OC)=CC32)C(Cl)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • 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:
LDDN-0003499
Cat. No.:
HY-112369
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