DPP-9
Dipeptidyl peptidase 9 (DPP9) is a cytosolic post-proline serine protease that functions as a key endogenous regulator of innate immune homeostasis through control of inflammasome signaling pathways[1]. Mechanistically, DPP9 directly interacts with the function-to-find domain (FIIND) of NLRP1 and contributes to maintenance of NLRP1 in an inactive state through both its peptidase activity and scaffolding function[1]. This regulatory mechanism suppresses downstream inflammasome activation, thereby limiting caspase-1 activation, interleukin-1β maturation, and pyroptotic cell death[1][2]. In disease-associated contexts, disruption of the DPP9-NLRP1 interaction, including germline mutations that impair FIIND-dependent binding, results in inflammasome hyperactivation and is linked to autoinflammatory disorders[1]. Structural studies further demonstrated that DPP9 sequesters the bioactive C-terminal fragment of NLRP1 and functions as a checkpoint that restrains spontaneous inflammasome activation[2]. Compared with the closely related isoform DPP8, DPP9 has been extensively characterized as a direct binding partner and negative regulator of both NLRP1 and CARD8 inflammasome sensors, highlighting a distinct role in inflammasome control beyond shared enzymatic activity[1][3]. For experimental applications, pharmacological DPP8/9 inhibitors, including Val-boroPro (VbP), disrupt DPP9-mediated repression and activate NLRP1- or CARD8-dependent inflammasome signaling, making these compounds valuable tools for studying inflammasome biology, pyroptosis, and inflammatory disease mechanisms[1][2][3].
References:
- [1]. Zhong FL, et al. Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. J Biol Chem. 2018 Dec 7;293(49):18864-18878. [Content Brief]
- [2]. Hollingsworth LR, et al. DPP9 sequesters the C terminus of NLRP1 to repress inflammasome activation. Nature. 2021 Apr;592(7856):778-783. [Content Brief]
- [3]. De Simone G, et al. Identification of a Kupffer cell subset capable of reverting the T cell dysfunction induced by hepatocellular priming. Immunity. 2021 Sep 14;54(9):2089-2100.e8. [Content Brief]
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DPP-9 Related Products (11)
Related Products (11)
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Anagliptin
0 ImagesSynonyms: SK-0403Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
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NZ-97
0 ImagesCat. No.: HY-158315Purity: 99.43%NZ-97 is a locally deliverable, lung-retaining dipeptidyl peptidase 4 (DPP4) inhibitor with an IC50 of 18 nM. It exhibits selectivity for DPP8 and DPP9 (with IC50 values of 1.3 μM and 0.6 μM, respectively). NZ-97 inhibits the DPP4 pool in lung-resident cells and epithelial lining fluid, elevates IL-6 and IGF-1 levels, and induces the expansion of type 2 alveolar epithelial cells (AEC2). NZ-97 reduces protein content in bronchoalveolar lavage fluid (BALF), ameliorates lung injury and alleviates pulmonary fibrosis. NZ-97 shows tolerability in untreated Mus musculus mice after intratracheal administration, and does not alter the proliferation or differentiation of lung fibroblasts. NZ-97 can be used in studies related to idiopathic pulmonary fibrosis, acute lung injury and emphysema.
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Anagliptin hydrochloride
0 ImagesCat. No.: HY-14877ACAS No.: 1359670-56-6Synonyms: SK-0403 hydrochlorideAnagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
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DPP9-IN-2
0 ImagesCat. No.: HY-179348CAS No.: 3020859-44-0DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection.
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DPP-8/9 probe-1
0 ImagesCat. No.: HY-D2327CAS No.: 3020859-80-4DPP-8/9 probe-1 (compound 20) is a fluorescent probe targeting Dipeptidyl Peptidase DPP8/9, which can be selectively labeled and visualized in vitro by fluorescence microscopy Active DPP8/9. DPP-8/9 probe-1 contains a nitrobenzoxadiazole (NBD) tag and has high affinity and selectivity for DPP8/9 over related S9 family members (IC50 of 210 nM and 15 nM, respectively).
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5-Hydroxy saxagliptin hydrochloride
0 ImagesCat. No.: HY-W741755A5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus.
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BMS-767778
0 ImagesCat. No.: HY-16656CAS No.: 915729-95-2BMS-767778 is an orally active and selective DPP4 inhibitor with Ki values of 0.94 nM, 4.9, 3.2 nM for DPP4, DPP8 and DPP9 respectively. BMS-767778 exhibits >3,000-fold selectivity over the related enzymes DPP8 and DPP9. BMS-767778 inhibits CYP-3A4 with IC50 of 5.2 μM. BMS-767778 significantly reduces blood glucose levels in high fat fed (HFD) ob/ob mice with safety profile. BMS-767778 can be used for diabetes mellitus research.
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DPP8/9-IN-1
0 ImagesCat. No.: HY-176001DPP8/9-IN-1 (Compound 16) is a selective covalent inhibitor of dipeptidyl peptidases 8 and 9 (DPP8/9) with IC50 values of 14 and 298 nM, respectively. DPP8/9-IN-1 binds irreversibly to the active site serine (S730 in DPP9) via a phosphonate warhead and blocks substrate binding to inhibit DPP8/9-mediated protein processing. DPP8/9-IN-1 is promising for research of cancers and inflammatory diseases.
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DPP9-IN-1
0 ImagesCat. No.: HY-172529CAS No.: 3020859-03-1DPP9-IN-1 (Compound 42) is a dipeptidyl peptidase 9 (DPP9) inhibitor with IC50 of 3 nM for DPP9 and 0.6 μM for DPP8. DPP9-IN-1 induces concentration-dependent LDH release in THP-1 cells.
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cis-ICeD-2
0 ImagesCat. No.: HY-151871Acis-ICeD-2 is the cis isomer of ICeD-2 (HY-151871). ICeD-2 is a cell death inducer that induces cell death in HIV-1-infected cells. ICeD-2-mediated killing of HIV-1-infected cells is dependent on HIV-1 protease activity. ICeD-2 effectively blocks the hydrolysis of Gly-Pro-AMC by the dipeptidyl peptidases DPP8 and DPP9. ICeD-2 demonstrates strong stability against DPP9 in PBMCs..
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DPP8/9-IN-2
0 ImagesCat. No.: HY-175226CAS No.: 3109603-86-0DPP8/9-IN-2 (Compound 21) is a DPP8/9 inhibitor with IC50 values of 0.22 nM and 3 nM, respectively, and Ki values of 2.9 nM and 6 nM, respectively . DPP8/9-IN-2 has certain cardiotoxicity, with IC50 values of 0.7 μM, 29.0 μM and 27.7 μM for hERG potassium channel, Nav1.5 sodium channel and Cav1.2 calcium channel, respectively. DPP8/9-IN-2 can be used in the research of diseases such as tumors.
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