2. Metabolic Enzyme/Protease
  3. Heme Oxygenase (HO)
  4. 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.

For research use only. We do not sell to patients.

KCL-HO-1i

KCL-HO-1i Chemical Structure

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KCL-HO-1i Related Antibodies

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Description

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[1].

IC50 & Target[1]

HO-1

123 nM (IC50, rat splenic microsomes )

HO-1

128 nM (IC50, HEK293T cells )

In Vitro

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.

KCL-HO-1i Related Antibodies
In Vivo

KCL-HO-1i (27.8 mg/kg (25 μMol/kg), p.o., daily, 21 days) alone slows tumor growth and synergizes with chemotherapy (5-fluorouracil (HY-90006) or Gemcitabine (HY-17026)) to deliver durable tumor growth control in MMTV-PyMT spontaneous breast cancer mice and C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: p.o., daily, 21 days
Administration: 25 μMol/kg, alone or combined with chemotherapy (5-fluorouracil (40 mg/kg/4 days) or Gemcitabine (6.6 mg/kg/7 days)
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.
Molecular Weight

1110.75

Formula

C34H36N4O12P2Sn3
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]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KCL-HO-1i Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KCL-HO-1iHeme Oxygenase (HO)Heme OxygenasecancerMMTV-PyMT spontaneous breast cancerMN-MCA1 sarcomasHO-1Inhibitorinhibitorinhibit

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