1. Signaling Pathways
  2. Immunology/Inflammation
  3. Kallikrein
  4. KLK1 Isoform

KLK1

Tissue kallikrein 1 (KLK1) is a serine protease primarily involved in the proteolytic release of vasoactive kinins, such as bradykinin, from precursor proteins in endothelial cells[1]. Mechanistically, KLK1 mediates vascular relaxation through the activation of bradykinin-dependent pathways, contributing to local cardiovascular regulation[1]. KLK1 expression is inducible in endothelial cells by angiotensin II, demonstrating its role in adaptive vascular responses[1]. In disease contexts, KLK1 administration enhances spermatogenesis recovery in busulfan-induced azoospermic mice, promoting proliferation of spermatogonial stem cells via ERK1/2 and cell cycle protein activation[2]. Transcriptomic analyses indicate that KLK1 is upregulated in high-altitude polycythemia, implicating it in hypertension and inflammatory responses through interactions with cholesterol[3]. Compared with other kallikrein family members, KLK1 possesses a distinctive endothelial and renal expression profile, with unique local effects on vasodilation and reproductive tissue regeneration[4][1][2]. Functionally, KLK1 serves as both a physiological regulator of vascular tone and a potential experimental target for reproductive and cardiovascular disease models[1][2][3]. Pharmacologically, KLK1 activity can be modulated using specific inhibitors or recombinant protein administration, facilitating experimental investigation of its role in vivo[1][2].

KLK1 Related Products (2):

Cat. No. Product Name Effect Purity
  • HY-148949A
    Kallikrein 5-IN-2 TFA
    Inhibitor 99.53%
    Kallikrein 5-IN-2 TFA is the TFA salt form of Kallikrein 5-IN-2 (HY-148949). Kallikrein 5-IN-2 TFA is a selective inhibitor for kallikrein 5 (KLK5) with pIC50 of 7.1. Kallikrein 5-IN-2 TFA is non-phototoxic (100 μg/mL) and non-irritant. Kallikrein 5-IN-2 is stable at pH 4-pH 8 under non-oxidative condition. Kallikrein 5-IN-2 is potent in ameliorating the Netherton syndrome.
  • HY-182600
    KLK6-IN-1
    Inhibitor
    KLK6-IN-1 is a reversible small‑molecule inhibitor of KLK6, KLK1, and plasmin. KLK6-IN-1 shows IC50 values of 1.57 μM (KLK6), 5.1 μM (KLK1), 7.4 μM (plasmin), and Ki values of 0.8 μM (KLK6), 2.4 μM (KLK1), 1.3 μM (plasmin). KLK6-IN-1 is highly selective for KLK6 and its proteolytic network. KLK6-IN-1 induces oligodendrocyte differentiation by promoting oligodendrocyte precursor cell maturation. KLK6-IN-1 can be used for the research of multiple sclerosis.