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Art. -Nr.: HY-185207

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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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3034207-17-2
Formel: C₁₉H₃₅N₃O₅
Molecular Weight:385.50

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

CQ80 Chemical Structure

CAS. Nr.: 3034207-17-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	0.27 μM Compound: CQ80; 14p	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	[PMID: 36724486]

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

Chemical Information

CAS. Nr. 3034207-17-2
Molecular Weight 385.50
Formel C₁₉H₃₅N₃O₅
SMILES

CC(C[C@H](NC([C@@H]1CCCN1C([C@H]([C@@H](CC(C)C)N)O)=O)=O)C(OC)=O)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen Q, et al. Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation. J Med Chem. 2023 Feb 23;66(4):2589-2607.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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