keratinocyte

Tracheloside significantly decreases the activity of alkaline phosphatase (IC50: 0.31 μg/ml), a level of inhibition comparable to that of tamoxifen (IC50: 0.43 μg/ml).

TB-500 is a synthesised peptide, essentially a short-chain version of the naturally occurring Thymosin Beta-4.

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

Casein Kinase II Inhibitor IV is an inducer of epidermal keratinocyte differentiation.

Myristoyl Tetrapeptide-12 Acetate (Myristoyl Tetrapeptide-12 Acetate (959610-24-3 Free base)) , the reaction product of myristic acid and Tetrapeptide-12, is a peptide stimulating hair and eyelash growth and enhancing the appearance of eyelashes and/or eyebrows. Myristoyl tetrapeptide-12 can increase keratinocyte proliferation improve appearance, firmness elasticity, and skin thickness.

Casein Kinase II Inhibitor IV Hydrochloride is a small-molecule inducer of epidermal keratinocyte differentiation, offering novel therapeutic approaches for treating skin hyperproliferative disorders.

Phenformin (BRN 1977317) is a biguanide compound with anticancer and anti-glycemic activity, inhibits skin tumor growth and promotes keratinocyte differentiation and apoptosis.

SK2220691 is a potent TRPV4 inhibitor. It effectively suppresses pulmonary edema induced by GSK1016790. Additionally, SK2220691 inhibits the increase of crucial factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF) induced by hydrochloric acid.

Lithocholic amide-C2-N(didecane) (Compound LC10) is a derivative of lithocholic acid. This compound spontaneously forms lipid nanoparticles in aqueous environments, allowing it to penetrate the skin and reach the dermis, where it exerts anti-inflammatory effects on psoriasis-like chronic skin inflammation. Lithocholic amide-C2-N(didecane) inhibits abnormal keratinocyte proliferation, downregulates the mRNA expression of the psoriasis-related receptor EphA2, and reduces serum levels of various pro-inflammatory factors (such as IL-1α, IL-1β, and IFN-γ) by inhibiting the activation of the Th17/Th2 inflammatory pathways.

CAY10583 is a potent and selective BLT2 (leukotriene B4 receptor type 2) agonist that increases TGF-β1 and bFGF expression, promotes keratinocyte migration and fibroblast proliferation, and accelerates wound healing in diabetic mice.

K6PC-5 is a ceramide derivative that acts as an activator of sphingosine kinase 1 (SPHK1), inducing a swift and temporary rise in intracellular calcium levels. With its potential applications in skin diseases associated with abnormal keratinocyte function, as well as in studies on neurodegeneration and virus infection, K6PC-5 presents a promising compound for research purposes.

BMS-480404 is an effective small molecule inhibitor, which can bind to human keratinocyte fatty acid-binding protein.

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)

(1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3), a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3), exerts potent actions through vitamin D receptor (VDR) activation, including the inhibition of keratinocyte growth and suppression of parathyroid hormone secretion [1].

1-O-Hexadecyl-sn-glycerol is a biologically active alkyl glyceryl ether that exhibits protective effects against UVB-induced cellular damage by reducing keratinocyte death, reactive oxygen species (ROS) generation, and prostaglandin E2 synthesis in normal human epidermal keratinocytes (NHEKs). additionally, at a concentration of 50 μM, 1-O-Hexadecyl-sn-glycerol significantly enhances coronary flow and left ventricular developed pressure while reducing malondialdehyde (MDA) formation in an ex vivo rat heart model of ischemia and reperfusion injury, thereby demonstrating both cytoprotective and cardioprotective properties.

PAR2 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth in the presence and absence of growth factors. PAR2 (1-6) inhibits LPS-induced pulmonary neutrophil influx and increases in matrix metalloproteinase-2 (MMP-2) activity in mice.

8(S)-HETE, a major lipoxygenase product in PMA-treated murine epidermis, activates mouse keratinocyte protein kinase C with an IC50 of 100 μM and selectively activates PPARα at concentrations as low as 0.3 μM. The stereochemical assignment of the (S) enantiomer is based on comparison of chiral HPLC retention times to published results.

Aureusimine B, also known as phevalin, is a natural pyrazinone produced by certain fungi and by Staphylococcus spp., including S. aureus. Its synthesis appears to be initiated by a conserved nonribosomal peptide synthetase that creates a dipeptide (phenylalanine-valine) aldehyde, which then undergoes cyclization and oxidation. Aureusimine B inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 μM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

4-Methyl-1-pentanol exhibits inhibitory activity against SCC-25 cells and NHK cells (normal human keratinocytes), making it useful for cancer research.

Antiproliferative agent-6 (compound 8a) is a potent antitumor compound exhibiting antiproliferative activity. It inhibits cancer cell lines HCT116, MCF-7, H460, and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50 values of 0.5 μM, 2 μM, 0.7 μM, and 3.5 μM, respectively.

NVS-BET-1 is a BET bromodomain inhibitor that can regulate keratinocyte plasticity.

Tazarotene (Zorac) is a synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.

Q-Peptide, an angiopoietin-1 derived peptide (QHREDGS), enhances keratinocyte migration, thereby facilitating wound healing in a diabetic mouse model, and accelerates wound closure [1].

Palmitoyl tetrapeptide-10 is a bioactive peptide that works synergistically with other active ingredients to increase the expression of corneodesmosin (a marker of keratinocyte adhesion) and filaggrin (a marker of keratinocyte terminal differentiation), thereby reducing skin permeability and improving skin barrier function. Palmitoyl tetrapeptide-10 can be used in research on sensitive skin syndrome and skin pigmentation.