KB528
KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC50 values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma.
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- No. CAS: 3082090-83-0
- Fòrmula: C28H28N6O
- Peso molecular:464.56
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
KB528 (0-1 μM; 24-72 h) selectively induces apoptosis in MM1.S cells in a concentration-dependent manner after 48 h of treatment[1].
KB528 (100 nM; 6-24 h) induces rapid loss of IKZF3 protein acetylation in MM1.S cells, followed by a transient decrease in mRNA, subsequent protein loss, and final rebound of mRNA levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1.S cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24, 48 and 72 h
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Result:First induced cell cycle arrest in the treatment for 24 hours, followed by apoptosis.
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Cell Line:MM1.S cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Potently and almost completely downregulated the mRNA of IRF4 and its target genes and the inhibition of IKZF1 and IKZF3 is relatively mild.
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Cell Line:MM1.S cells
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Concentration:100 nM
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Incubation Time:6 and 14 h
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Result:Significantly reduced the levels of MYC, IRF4, and IKZF3 proteins, and notably, the protein loss of IKZF3 was more significant than the decrease in its mRNA.
Chemical Information
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No. CAS 3082090-83-0
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Peso molecular 464.56
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Fòrmula C28H28N6O
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SMILES
N#CC1=CC=C([C@H](C)CN[C@H](C2=CC=CC=C2)[C@@H]3CNC4=C(N=CC(C5=CN(C)N=C5)=C4)O3)C=C1
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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)
KB528 Related Classifications
HY-181957 Related Classifications
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