KPV

preclinical

Also known as: Lysine-Proline-Valine, α-MSH (11-13)

**Mechanism of Action** KPV (Lysine-Proline-Valine), the C-terminal tripeptide of α-melanocyte-stimulating hormone (α-MSH 11-13), exerts anti-inflammatory effects primarily through PepT1-mediated cellular uptake. Once internalized, it inhibits nuclear factor-κB (NF-κB) activation, reducing pro-inflammatory cytokine production (e.g., TNF-α, IL-1β, IL-6). This pathway is particularly relevant in intestinal epithelial cells and immune cells, where KPV modulates oxidative stress and apoptosis. **Key Research Findings** Preclinical studies in inflammatory bowel disease (IBD) models (e.g., DSS-induced colitis in mice) demonstrate that KPV reduces colonic inflammation, mucosal damage, and neutrophil infiltration. It also enhances tight junction protein expression (e.g., occludin, ZO-1), improving intestinal barrier integrity. In vitro, KPV suppresses LPS-induced NF-κB signaling in Caco-2 cells and macrophages. Notably, its effects are dose-dependent and require PepT1 expression, as PepT1 knockout models show diminished efficacy. **Clinical Relevance** KPV remains in preclinical development, with no human trials reported. Its potential lies in targeted therapy for IBD, particularly ulcerative colitis and Crohn’s disease, where PepT1 is upregulated in inflamed tissue. However, challenges include rapid enzymatic degradation and limited oral bioavailability. Future research may focus on formulation strategies (e.g., nanoparticle encapsulation) to enhance stability and delivery. For research purposes only — not medical advice.

Key data

Category
Healing & Recovery
Molecular weight
192.21 g/mol
Molecular formula
C11H12O3
CAS number
88768-11-0
Administration
oral, subcutaneous, topical
Research status
preclinical
References
88
Tags
anti-inflammatory, gut-health, melanocortin

Research & studies

NLRP3 autophagic degradation disruption in melanocytes contributes to vitiligo development
Cell death and differentiation · 2026 · PubMed

NLRP3 expression is significantly increased in melanocytes of vitiligo patients and melanoma-Treg-induced vitiligo mice.; Knockout of NLRP3 effectively alleviates vitiligo progression in the mouse model.; Downregulation of β-TrCP1 reduces K27-linked ubiquitination of NLRP3, weakening its interaction with autophagy receptor NDP52 and impairing selective autophagic degradation.; Melanocyte-specific knockdown of NLRP3 using KPV-Lipos with Nlrp3 shRNA significantly alleviates vitiligo development.

Inflammation-triggered self-immolative conjugates enable oral peptide delivery by overcoming gastrointestinal barriers
Science advances · 2026 · PubMed
Lysine-Proline-Valine peptide mitigates fine dust-induced keratinocyte apoptosis and inflammation by regulating oxidative stress and modulating the MAPK/NF-κB pathway
Tissue & cell · 2025 · PubMed

PM10 exposure suppressed HaCaT cell proliferation and induced IL-1 secretion.; KPV (50 μg/mL) restored cell viability and reduced IL-1 secretion in PM10-treated cells.; KPV inhibited ROS production and suppressed MAPK (ERK, p38) activation and NF-κB signaling.; KPV decreased apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3) and blocked ROS-mediated caspase-1 activation, reducing IL-1 secretion.

Vimentin is required for tumor progression and metastasis in a mouse model of non-small cell lung cancer
Oncogene · 2023 · PubMed

Vimentin knockout (KPV-/-) mice showed attenuated tumor growth and improved survival compared to controls.; Therapeutic disruption of vimentin with withaferin A suppressed tumor growth and reduced lung tumor burden.; Mature vimentin intermediate filaments are required for cell-autonomous metastasis.; Vimentin loss upregulates ferroptosis genes, reduces GPX4, and increases toxic lipid peroxides.

Transdermal Iontophoretic Delivery of Lysine-Proline-Valine (KPV) Peptide Across Microporated Human Skin
Journal of pharmaceutical sciences · 2017 · PubMed
Peptide Receptor-Targeted Fluorescent Probe: Visualization and Discrimination between Chronic and Acute Ulcerative Colitis
ACS applied materials & interfaces · 2017 · PubMed

DCM-KPV specifically targets PepT1 overexpressed in chronic ulcerative colitis epithelial cells.; The probe exhibits long emission, low photobleaching, negligible cytotoxicity, and high cytocompatibility.; It enables direct noninvasive observation of colon inflammation and distinguishes chronic, acute, and normal groups.; The method provides real-time tracking of intracellular KPV, replacing time-consuming and invasive H&E staining.

Drug-loaded nanoparticles targeted to the colon with polysaccharide hydrogel reduce colitis in a mouse model
Gastroenterology · 2010 · PubMed

NPs (400 nm) did not affect cell viability or barrier functions.; Alginate-chitosan hydrogel containing NPs collapsed in the colon, enabling targeted delivery.; NP-KPV reduced inflammatory responses in Caco2-BBE cells in a dose-dependent manner.; Mice given DSS and NP-KPV were protected against inflammatory and histologic damage compared to DSS-only controls.

Terminal signal: anti-inflammatory effects of α-melanocyte-stimulating hormone related peptides beyond the pharmacophore
Advances in experimental medicine and biology · 2010 · PubMed

Frequently asked questions

What is KPV?

**Mechanism of Action** KPV (Lysine-Proline-Valine), the C-terminal tripeptide of α-melanocyte-stimulating hormone (α-MSH 11-13), exerts anti-inflammatory effects primarily through PepT1-mediated cellular uptake. Once internalized, it inhibits nuclear factor-κB (NF-κB) activation, reducing pro-inflammatory cytokine pro

How does KPV work?

C-terminal tripeptide of α-MSH with anti-inflammatory action via PepT1 uptake and NF-κB inhibition, studied in IBD models.

What is the research status of KPV?

KPV is currently classified as preclinical, with 88 research references on record. This is for research purposes only and is not medical advice.

What is the molecular weight of KPV?

KPV has a molecular weight of approximately 192.21 g/mol (formula C11H12O3).

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