1. Apoptosis Immunology/Inflammation
  2. Pyroptosis
  3. 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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CQ80

CQ80 Chemical Structure

CAS No. : 3034207-17-2

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Description

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)[1].

In Vitro

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.

Cell Viability Assay[1]

Cell Line: MV4-11 WT cells, MV4-11 CASP1⁻/⁻ cells, OCI-AML2 cells
Concentration: 100 μM to 15.2 nM (three-fold dilutions)
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: THP-1 cells, THP-1 PEPD/XPNPEP1⁻/⁻ cells, MV4-11 cells, OCI-AML2 cells, human resting T cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Detected GSDMD cleavage bands, while no such bands were found in THP-1 PEPD/XPNPEP1⁻/⁻ cells

Western Blot Analysis[1]

Cell Line: HEK293T CASP1+GSDMD cells
Concentration: 20 μM
Incubation Time: 6 h
Result: GSDMD cleavage bands were detected in HEK293T cells after combined treatment with dTAG-13
Molecular Weight

385.50

Formula

C19H35N3O5

CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.

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