KCL-HO-1i
KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC50 = 123 nM) and human HO-1: IC50 = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1+ perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C34H36N4O12P2Sn3
- Peso molecular:1110.75
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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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Help & FAQs
Actividad biológica
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HO-1 123 nM (IC50, rat splenic microsomes ) |
HO-1 128 nM (IC50, HEK293T cells ) |
KCL-HO-1i exhibits inhibitory activity against rat heme oxygenase-1 (HO-1) in rat splenic microsomes (IC50 = 123 nM) and HEK293T cells (IC50 = 128 nM)[1].
KCL-HO-1i (25 μM, 16 h) improves transendothelial migration of CD8+ T-cells, reversing the migration restriction caused by IL-6-polarized bone marrow-derived macrophages in a transwell assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Transgenic MMTV-PyMT mice (FVB/N background) with spontaneous breast tumor development or MN-MCA1 sarcoma cells (2.5 × 105 in 100 µL RPMI 1640) were subcutaneously implanted into the flanks of 21-25 g female C57Bl/6 mice to establish ectopic sarcoma tumorsMN-MCA1 sarcoma cells (2.5 × 10⁵ in 100 µL RPMI 1640) were subcutaneously implanted into the flanks of 21-25 g female C57Bl/6 mice to establish ectopic sarcoma tumors[1]
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Dosage:p.o., daily, 21 days
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Administration:25 μMol/kg, alone or combined with chemotherapy (5-fluorouracil (40 mg/kg/4 days) or Gemcitabine (6.6 mg/kg/7 days)
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Result:Achieved tumor growth control.
Caused mild pulmonary inflammation (grade 2-3) in mice.
Reduced the expression of TIM3 (an inhibitory immune checkpoint receptor) on CD8+ T-cells.
Chemical Information
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Peso molecular 1110.75
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Fòrmula C34H36N4O12P2Sn3
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SMILES
CCC1=C(C)C2=N/C1=C\C3=C(C)C(CC)=C4N3[Sn](OP([O-])([O-])=O)(OP([O-])([O-])=O)N(/C(C(C)=C/5CCC(O)=O)=C\2)C5=C/C6=N/C(C(C)=C6CCC(O)=O)=C\4.[Sn+2].[Sn+2]
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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)
KCL-HO-1i Related Classifications
HY-175660 Related Classifications
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