JH-IX-179
JH-IX-179 is an FLT3 inhibitor (IC50 = 4 nM (FLT3-ITD), 10 nM (FLT3-D835Y)). JH-IX-179 inhibits G1 phase arrest and induces apoptosis in FLT3-ITD-expressing cells. JH-IX-179 can be used in acute myeloid leukemia (AML) research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1939104-08-1
- Formel: C26H24N6O
- Molecular Weight:436.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
10 nM
Compound: 4; JH-IX-179
|
Inhibition of FLT3 ITD mutant (unknown origin) transduced in mouse Ba/F3 cells assessed as reduction in cell viability after 3 days by cell titer glo assay
Inhibition of FLT3 ITD mutant (unknown origin) transduced in mouse Ba/F3 cells assessed as reduction in cell viability after 3 days by cell titer glo assay
|
[PMID: 27190596] |
| BaF3 | IC50 |
4 nM
Compound: 4; JH-IX-179
|
Inhibition of FLT3 D835Y mutant (unknown origin) transduced in mouse Ba/F3 cells assessed as reduction in cell viability after 3 days by cell titer glo assay
Inhibition of FLT3 D835Y mutant (unknown origin) transduced in mouse Ba/F3 cells assessed as reduction in cell viability after 3 days by cell titer glo assay
|
[PMID: 27190596] |
| MOLM-13 | IC50 |
2 nM
Compound: 4; JH-IX-179
|
Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as reduction in cell viability a after 3 days by cell titer glo assay
Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as reduction in cell viability a after 3 days by cell titer glo assay
|
[PMID: 27190596] |
| MOLM-14 | IC50 |
11 nM
Compound: 4; JH-IX-179
|
Inhibition of FLT3 ITD mutant in human MOLM14 cells assessed as reduction in cell viability after 3 days by cell titer glo assay
Inhibition of FLT3 ITD mutant in human MOLM14 cells assessed as reduction in cell viability after 3 days by cell titer glo assay
|
[PMID: 27190596] |
Chemical Information
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CAS. Nr. 1939104-08-1
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Molecular Weight 436.51
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Formel C26H24N6O
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SMILES
O=C1C2=C(C(N3)=C1C4=C3C=C(C5=CNN=C5)C=C4)C=C(C6=CN(CCCN(C)C)N=C6)C=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)