P300-IN-6
P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma.
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- CAS No.: 3034595-62-2
- 화학식: C26H26N6O2
- 분자량:454.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
p300-HAT 7 nM (IC50) |
In Vitro
P300-IN-6 (Compound B6) potently inhibits the recombinant human p300 HAT domain with an IC50 of 7 nM[1].
P300-IN-6 potently inhibits the proliferation of human multiple myeloma OPM-2 cells with an IC50 of 8.8 nM[1].
P300-IN-6 (100 nM; 6 days) inhibits the proliferation of human prostate cancer 22RV1 cells, achieving 70-80% growth inhibition at 100 nM[1].
P300-IN-6 (1-20 nM; 24 h) dose-dependently suppresses c-Myc expression and reduces H3K18ac/H3K27ac levels in OPM-2 and 22RV1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OPM-2 cells，22RV1 cells
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Concentration:1, 5, 10, 15, 20 nM
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Incubation Time:24 h
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Result:Dose-dependently suppressed c-Myc expression as early as 6 h, and c-
Myc remained markedly suppressed through 12-24 h.
Reduced H3K18ac and H3K27ac levels.
Showed active inhibitory effect at 5-10 nM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 6 weeks old)[1]
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Dosage:20 mg/kg
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Administration:I.g.; once daily; 17 consecutive days
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Result:Achieved a tumor growth inhibition (TGI) value of 60%.
Showed good tolerability, with no mortality and only a slight decrease in body weight over the dosing period.
Chemical Information
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CAS No. 3034595-62-2
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분자량 454.52
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화학식 C26H26N6O2
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SMILES
CN1C2=CC=C(NC([C@@H](C3=CC=CC=C3)NC[C@@H](C)C4=CC=C(C#N)C=C4)=O)N=C2N(C)C1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P300-IN-6 Related Classifications
HY-181669 Related Classifications
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