JQKD82
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form that retains the same biological activity.
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- No. CAS: 2410512-38-6
- Fòrmula: C27H40N4O5
- Peso molecular:500.63
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
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KDM5 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | EC50 |
0.42 μM
Compound: 48
|
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
|
[PMID: 34555614] |
In Vitro
JQKD82 (0.3 μM; 24 hours) causes an increase in the global H3K4me3 level of MM.1S cells[1].
JQKD82 (0.1-10 μM; day 1-day 5) inhibits the growth of MM.1S cells in a dose- and time-dependent manner. JQKD82 is potent at eliciting growth suppression in MM.1S cells (IC50=0.42 μM)[1].
JQKD82 (1 μM; 24 hours) induces G1 cell-cycle arrest by 48 hours in MM.1S and MOLP-8 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
JQKD82 displays an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (bearing MOLP-8 TurboGFP-Luc cells)[1]
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Dosage:50 mg/kg, 75 mg/kg
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Administration:i.p.; twice a day for 3 weeks
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Result:Significantly reduced tumor burden.
Chemical Information
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No. CAS 2410512-38-6
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Peso molecular 500.63
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Fòrmula C27H40N4O5
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SMILES
O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OC2=CC=C(C=C2OC(C)C)OC(C)C
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Synonyms
JADA82; PCK82
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)