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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- CAS 番号: 441022-67-9
- 分子式: C13H24N2O4
- 分子量:272.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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Caspase-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
2.2 μM
Compound: CQ31; 10a
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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] |
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.
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Cell Line:Wild-type MV4;11 cells, CASP1 knockout MV4;11 cells
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Concentration:0.0152-100 μM, three-fold dilution
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Incubation Time:24 h
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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.
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Cell Line:MV4;11, OCI-AML2, THP-1 cells, primary human resting T cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Induced GSDMD cleavage.
化学情報
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CAS 番号 441022-67-9
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分子量 272.34
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分子式 C13H24N2O4
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SMILES
CC(C)C[C@@H](N)[C@H](O)C(N1[C@@H](CCC1)C(OC)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)