CQ80
CQ80 is a PEPD/XPNPEP1 inhibitor and selective CARD8 inflammasome activator. CQ80 has IC50 values of 0.91 μM for PEPD, 43 μM for XPNPEP1. CQ80 promotes the accumulation of Xaa-Pro peptides by inhibiting PEPD and XPNPEP1, releases the fragment of CARD8 for inflammasome formation, and induces pyroptosis via GSDMD cleavage. CQ80 can be used for research on inflammasome, CARD8-expressing cancer cells, HIV-1-infected cell clearance, acute myeloid leukemia (AML).
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- No. CAS: 3034207-17-2
- Fòrmula: C19H35N3O5
- Peso molecular:385.50
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
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| MV4-11 | IC50 |
0.27 μM
Compound: CQ80; 14p
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Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 24 hrs by celltiter-glo assay
Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 24 hrs by celltiter-glo assay
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[PMID: 36724486] |
CQ80 (0.15 nM-100 μM; 24 h) induces CASP1-dependent pyroptosis in MV4-11 cells with an IC50 of 0.27 μM, and shows potent cytotoxicity against OCI-AML2 cells[1].
CQ80 (6.25 μM; 6 h) promotes Propidium Iodide (PI) (HY-D0815) uptake in MV4-11 and OCI-AML2 cells, indicating lytic cell death[1].
CQ80 (20 μM; 24 h) induces lactate dehydrogenase (LDH) release and gasdermin D (GSDMD) cleavage in MV4-11, OCI-AML2, THP-1 cells and human resting T cells[1].
CQ80 (20 μM; 24 h) shows no activity in N/TERT-1 keratinocytes, mouse bone marrow-derived macrophages (BMDMs) and RAW264.7 cells, failing to activate NLRP1 inflammasome[1].
CQ80 (20 μM; 24 h) does not induce additional pyroptosis in DPP8/9 knockout THP-1 cells, and PEPD/XPNPEP1 double knockout THP-1 cells are completely resistant to CQ80[1].
CQ80 (20 μM; 6 h) disrupts the CARD8-DPP9 ternary complex in HEK293T cells stably expressing CASP1 and GSDMD[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 WT cells, MV4-11 CASP1⁻/⁻ cells, OCI-AML2 cells
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Concentration:100 μM to 15.2 nM (three-fold dilutions)
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Incubation Time:24 h
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Result:Induced CASP1-dependent cell death in MV4-11 WT cells, with no such effect in MV4-11 CASP1⁻/⁻ cells.
Exhibited higher cytotoxicity against OCI-AML2 cells compared to CQ31.
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Cell Line:THP-1 cells, THP-1 PEPD/XPNPEP1⁻/⁻ cells, MV4-11 cells, OCI-AML2 cells, human resting T cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Detected GSDMD cleavage bands, while no such bands were found in THP-1 PEPD/XPNPEP1⁻/⁻ cells
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Cell Line:HEK293T CASP1+GSDMD cells
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Concentration:20 μM
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Incubation Time:6 h
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Result:GSDMD cleavage bands were detected in HEK293T cells after combined treatment with dTAG-13
Chemical Information
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No. CAS 3034207-17-2
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Peso molecular 385.50
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Fòrmula C19H35N3O5
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SMILES
CC(C[C@H](NC([C@@H]1CCCN1C([C@H]([C@@H](CC(C)C)N)O)=O)=O)C(OC)=O)C
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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)
CQ80 Related Classifications
HY-185207 Related Classifications
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- CQ80
- 3034207-17-2
- CQ 80
- CQ-80
- Pyroptosis
- PEPD/XPNPEP1 inhibitor
- selective CARD8 inflammasome activator
- induces pyroptosis
- MV4-11 cells
- OCI-AML2 cells
- THP-1 cells
- HEK 293T cells
- RAW264.7 cells
- human resting T cells
- mouse bone marrow-derived macrophages (BMDMs)
- acute myeloid leukemia (AML)
- HIV-1 infection
- inflammasome
- Inhibitor
- inhibitor
- inhibit