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MilliporeSigma™ Calbiochem™ Val-boroPro

Catalog No. 5314650001 Shop All MilliporeSigma Products
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53-146-50001 10 mg
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Catalog No. 53-146-50001 Supplier MilliporeSigma™ Supplier No. 5314650001
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Description

An orally available amino boronic acid dipeptide with antihyperglycemic and anticancer properties

An orally available amino boronic acid dipeptide with antihyperglycemic and anticancer properties. Acts as a highly potent, reversible, and transition state analog inhibitor of dipeptidyl peptidase IV (DPP-IV; IC50 = 26nM; Ki = 180 pM). Also inhibits the activity of other prolyl peptidases (IC50 = 15nM for DPP-II; and Ki = 1.5nM and 760 pM for DPP8 and DPP9, respectively) and at much higher concentrations affects the activities of quiescent cell proline dipeptidase (QPP, DPP7; IC50 = 310nM), PEP (IC50 = 390nM) and fibroblast activation protein (FAP; IC50 = 560nM). However, it does not inhibit the activity of trypsin, chymoptrypsin, thrombin, plasmin, tryptase, leukocyte elastase, and plasma kallikrein even at high levels (∽100μM). Promotes hematopoiesis and the growth of primitive hematopoietic progenitor cells by increasing the production of G-CSF, IL-6, and IL-11 by bone marrow stromal cells in mice. Although it has no direct cytotoxic effect on tumors in vitro, but oral administration in mice is shown to reduce the growth of syngeneic tumors derived from fibrosarcoma (WEHI164), lymphoma (EL4 and A20/2J), melanoma (B16-F10), and mastocytoma (P815) cell lines and augments antibody-dependent cell-mediated cytotoxicity. Note: In aqueous physiological solutions, it can cyclize in a time-dependent manner causing a 100-fold diminution in its inhibitory potency. However, at lower pH range it remains in an active open chain form. Maximum tolerated dose in mice or rats is ∽ 25μg/kg.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
TRUSTED_SUSTAINABILITY

Specifications

Color Light Beige
Description 98% by HPLC
Target Proteins DPP-IV, DPP8 and DPP9
CAS 150080-09-4
Molecular Formula C10H23BN2O6S
Solubility DMSO
Content And Storage Hygroscopic, Protect from light
Form Solid
Quantity 10 mg
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