BM-51
BM-51 is a selective inhibitor of CYP4Z1, with a human IC50 value of 91.7 nM. BM-51 binds to amino acid residues of CYP4Z1, thereby inhibiting its enzymatic activity. BM-51 downregulates the protein expression of stem cell markers (ALDH1A1, SOX2, OCT3/4 and KLF4) in cancer cells, inhibits cancer cell migration and invasion, and exhibits low toxicity to normal cells/tissues. BM-51 suppresses tumor initiation capacity and enhances the chemotherapeutic efficacy of Doxorubicin (HY-15142A). BM-51 can be used in breast cancer-related research.
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- CAS. Nr.: 3038211-56-9
- Formel: C17H23N3O
- Molecular Weight:285.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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CYP4Z1 91.7 nM (IC50) |
ALDH1A1 |
KLF4 |
BM-51 potently inhibits the enzymatic activity of CYP4Z1 (IC50 = 91.7 nM)[1] by binding to the Arg384, Ser383, Val126 and Ala314 amino acid residues of CYP4Z1 in HEK293T cell lysates.
BM-51 (500 μM; 30 min) directly binds to the Arg384, Ser383, Val126 and Ala314 sites of CYP4Z1 in protein extracts[1].
BM-51 reduces the mammosphere-forming capacity (a tumor-initiating cell-like trait) of 4T1 cells overexpressing wild-type CYP4Z1, but exerts no such effect on cells overexpressing CYP4Z1Arg384, CYP4Z1Ser383, CYP4Z1Val126 or CYP4Z1Ala314[1].
BM-51 reduces the proportion of CD44+/CD24− tumor-initiating cell (TIC) subsets in 4T1 cells overexpressing wild-type CYP4Z1, but exerts no such effect on cells overexpressing CYP4Z1 with mutations at Arg384, Ser383, Val126 or Ala314[1].
BM-51 (0.01-100 μM; 72 h) shows no significant inhibitory effect on cell viability in MCF-7, MDA-MB-231 and 4T1 cells[1].
BM-51 (0.25-10 μM; 24-48 h) exhibits significant inhibitory effects on cell migration in MCF-7 and MDA-MB-231 cells [1].
BM-51 (0.25-10 μM) downregulates the protein expression levels of stem cell markers ALDH1A1, SOX2, OCT3/4 and KLF4 in MCF-7 and MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, MDA-MB-231, 4T1 cells
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Concentration:0.01, 0.1, 1, 10 and 100 μM
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Incubation Time:72 h
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Result:Did not significantly inhibit cell viability in MCF-7, MDA-MB-231, and 4T1 cells, with an IC50 > 20 μM
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Cell Line:MCF-7 and MDA-MB-231 cells
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Concentration:0.25, 1.0 μM (MDA-MB-231 cells); 2.5, 10 μM(MDA-MB-231 cells)
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Incubation Time:24 h (MDA-MB-231 cells); 48 h(MDA-MB-231 cells)
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Result:Wound healing and Transwell invasion assays (with Matrigel coating) demonstrated significant inhibition of cell migration and invasion in MCF-7 and MDA-MB-231 cells.
BM-51 (10 mg/kg; daily; for 14 consecutive days) enhances the chemotherapeutic efficacy of Doxorubicin (HY-15142A) against MCF-7 breast cancer xenografts, inhibits tumor stemness, and exhibits low toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female; PyMT-CYP4Z1 and PyMT-MMTV genotypes; spontaneous breast cancer tumorigenesis model)[1]
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Dosage:10 mg/kg
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Administration:i.v.; every 3 days; 6 weeks
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Result:Significantly delayed tumor initiation in PyMT-CYP4Z1 mice.
Reduced tumor size, count, volume, and weight in PyMT-CYP4Z1 mice.
Decreased the number and size of metastatic lung nodules in PyMT-CYP4Z1 mice.
Reduced the number and size of hyperplastic mammary gland lesions at 15 weeks in PyMT-CYP4Z1 mice.
Decreased the proportion of luminal progenitor (CD29^lo CD24^+) cells in PyMT-CYP4Z1 mice.
Increased the proportion of basal (CD29^+ CD24^+) cells in PyMT-CYP4Z1 mice.
Had no effect on mammary gland development in normal wild-type mice.
Modestly reduced common myeloid progenitor (CMP) bone marrow subsets in normal wild-type mice.
Caused no notable changes in other hematopoietic progenitor subsets or peripheral blood cell counts in normal wild-type mice.
Left PyMT mRNA levels in PyMT-CYP4Z1 tumors unchanged.
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Animal Model:BALB/c nude (male; 6 weeks old; MCF-7 cell subcutaneous xenograft model)[1]
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Dosage:10 mg/kg
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Administration:daily; 14 days
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Result:Did not significantly suppress tumor progression when used alone compared with control.
Enhanced the tumor-suppressive effects of Adriamycin, resulting in reduced tumor weight and volume relative to Adriamycin alone.
Did not alter mouse body weight, indicating low toxicity.
Suppressed the expression of stemness markers in tumors.
Chemical Information
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CAS. Nr. 3038211-56-9
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Molecular Weight 285.38
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Formel C17H23N3O
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SMILES
O=C(NC(C)CCC)CC1=CC=C(CN2C=NC=C2)C=C1
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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)