hCYP1B1-IN-2
hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM.
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- CAS. Nr.: 3043683-33-3
- Formel: C17H10BrN3O2
- Molecular Weight:368.18
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
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CYP1B1 0.040 nM (IC50) |
CYP1A1 0.38 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H460 | IC50 |
100.8 nM
Compound: 3n
|
Synergistic anti-cancer activity of human PTX-resistant NCI-H460 cells assessed as PTX IC50 at 5 uM incubated for 48 hrs in presence of PTX by CCK8 assay
Synergistic anti-cancer activity of human PTX-resistant NCI-H460 cells assessed as PTX IC50 at 5 uM incubated for 48 hrs in presence of PTX by CCK8 assay
|
[PMID: 38692523] |
In Vitro
hCYP1B1-IN-2 (compound 3n) (5 μM) can significantly reverse the Paclitaxel (PTX, HY-B0015) resistance in H460/PTX cells, evidenced by the dramatically reduced IC50 values, from 632.6 nM (PTX alone) to 100.8 nM (PTX plus 3n)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3043683-33-3
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Molecular Weight 368.18
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Formel C17H10BrN3O2
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SMILES
O=C(N(CC1=CN=CN=C1)C2=O)C3=CC=C(Br)C4=CC=CC2=C43
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)