1. Apoptosis Immunology/Inflammation
  2. Pyroptosis Caspase
  3. CQ31

CQ31 is a PEPD and XPNPEP1 inhibitor, with an IC50 of 0.67 μM against PEPD and an IC50 of 122 μM against XPNPEP1. CQ31 inhibits the M24B aminopeptidase activity of PEPD and XPNPEP1. CQ31 induces the accumulation of Xaa-Pro-containing peptides, mildly inhibits DPP8/9, and triggers CASP1-dependent pyroptosis via activation of the CARD8 inflammasome and caspase-1. CQ31 can be used in research related to cancers such as acute myeloid leukemia.

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CQ31

CQ31 Chemical Structure

CAS No. : 441022-67-9

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Description

CQ31 is a PEPD and XPNPEP1 inhibitor, with an IC50 of 0.67 μM against PEPD and an IC50 of 122 μM against XPNPEP1. CQ31 inhibits the M24B aminopeptidase activity of PEPD and XPNPEP1. CQ31 induces the accumulation of Xaa-Pro-containing peptides, mildly inhibits DPP8/9, and triggers CASP1-dependent pyroptosis via activation of the CARD8 inflammasome and caspase-1. CQ31 can be used in research related to cancers such as acute myeloid leukemia[1][2].

IC50 & Target[2]

Caspase-1

 

In Vitro

CQ31 (0.0152-100 μM; 24 h) induces CASP1-dependent cytotoxicity in wild-type MV4;11 cells with an IC50 of 3.8 μM, but exerts no cytotoxic effect on CASP1-knockout MV4;11 cells[1].
CQ31 (6.25 μM; 6 h) induces CARD8- and CASP1-dependent lytic cell death as well as caspase-1-dependent pyroptosis in wild-type MV4;11 cells, but exerts no such effects in CASP1-knockout or CARD8-knockout MV4;11 cells[1][2].
CQ31 (20 μM; 24 h) induces CARD8-dependent pyroptosis (cell death, LDH release, GSDMD cleavage) in wild-type OCI-AML2 and THP-1 cells, but shows no such effect in CARD8-knockout cells, and induces pyroptosis (GSDMD cleavage) in human primary resting T cells[1].
CQ31 (20 μM; 24 h) induces pyroptosis in THP-1 cells by inhibiting PEPD and XPNPEP1, which in turn suppresses downstream DPP8/9 and activates the CARD8 inflammasome[1].
CQ31 (20 μM; 6 h) disrupts the CARD8-DPP9 ternary complex, induces CARD8-dependent pyroptosis in HEK 293T cells analyzed by dTAG, and inhibits the enzymatic activity of DPP8/9 in HEK 293T cells[1][2].
CQ31 inhibits prolinase activity in THP-1 cell lysates in a dose-dependent manner, and completely blocks the cleavage of Ala-Pro dipeptide[2].
CQ31 (30 min) selectively stabilizes PEPD in HEK 293T cell lysates in CETSA assays, with no effect on DPP9 or NPEPPS[2].
CQ31 (10 μM; 24 h) induces pyroptosis in resting human primary T cells, which is evidenced by the cleavage of GSDMD[2].

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

Cell Cytotoxicity Assay[1]

Cell Line: Wild-type MV4;11 cells, CASP1 knockout MV4;11 cells
Concentration: 0.0152-100 μM, three-fold dilution
Incubation Time: 24 h
Result: Induced CASP1-dependent cytotoxicity in wild-type MV4;11 cells with an IC50 of 3.8 μM.
Showed no cytotoxicity (IC50 >100 μM) in CASP1 knockout MV4;11 cells.

Western Blot Analysis[1]

Cell Line: MV4;11, OCI-AML2, THP-1 cells, primary human resting T cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Induced GSDMD cleavage.
Molecular Weight

272.34

Formula

C13H24N2O4

CAS No.
SMILES

CC(C)C[C@@H](N)[C@H](O)C(N1[C@@H](CCC1)C(OC)=O)=O

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

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    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.

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