Signaling Pathway

DPP4

DPP4

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DPP4 is an antigenic enzyme expressed on the surface of most cell types and is associated with immune regulation,signal transduction and apoptosis. DPP4 is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides. The substrates of CD26/DPPIV are proline-containing peptides and include growth factors, chemokines, neuropeptides, and vasoactive peptides. DPP4 plays a major role in glucose metabolism. DPP4 is responsible for the degradation of incretins such as GLP-1. Furthermore, DPP4 appears to work as a suppressor in the development of cancer and tumours. CD26/DPPIV plays an important role in tumor biology, and is useful as a marker for various cancers, with its levels either on the cell surface or in the serum increased in some neoplasms and decreased in others.

DPP4 Inhibitors & Modulators (17)

Product Name Catalog No. Brief Description
Alogliptin

HY-A0023A

Alogliptin(SYR-322) is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.

Alogliptin Benzoate

HY-A0023

Alogliptin benzoate(SYR 322) is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.

Anagliptin

HY-14877

Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9.

DBPR108

HY-12528

DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.

Linagliptin

HY-10284

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

Omarigliptin

HY-15981

Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all
proteases tested (IC50 > 67 μM).

Saxagliptin

HY-10285

Saxagliptin is a drug which was developed for the treatment of respiratory disorders such as asthma and Chronic Obstructive Pulmonary Disease (COPD).

Saxagliptin hydrate

HY-10285A

Saxagliptin H2O(BMS477118 H2O) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.

Sitagliptin

HY-13749

Sitagliptin(MK 0431) is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Sitagliptin phosphate

HY-13749A

Sitagliptin phosphate(MK 0431 phosphate) is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Sitagliptin phosphate monohydrate

HY-13749B

Sitagliptin(MK 0431) phosphate monohydrate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Talabostat mesylate

HY-13233A

Talabostat mesilate(PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases(IC50=1 nM for DPP4), including tumor-associated fibroblast activation protein.

Teneligliptin

HY-14806

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Teneligliptin hydrobromide

HY-14806A

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Trelagliptin

HY-15408

Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).

Trelagliptin succinate

HY-15408A

Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).

Vildagliptin

HY-14291

Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.