Indole-3-pyruvic acid

Indole-3-pyruvic acid is an orally active ketone analog of tryptophan, and is an aryl hydrocarbon receptor (AHR) agonist. Indole-3-pyruvic acid inhibits p38/MAPK phosphorylation, regulates the tryptophan metabolic pathway, and also possesses protective activities against skin photodamage, as well as anti-inflammatory and anti-anxiety bioactivities in the gut. Indole-3-pyruvic acid can downregulate the expression of IL-1β, IL-6, Cox-2, and Bax to alleviate UVB-induced keratinocyte toxicity. Indole-3-pyruvic acid can activate AHR to promote Tr1 cell differentiation, increase IL-10, and inhibit Th1 cytokine production. Indole-3-pyruvic acid can alter the levels of kynurenine metabolites in the brain, mediating central nervous system-related effects. Indole-3-pyruvic acid can be used in research on skin lesions, colitis, and anxiety^[1][2][3]. IC50 & Target:AHR^[1] In Vitro:Indole‑3‑pyruvic acid (IPyr) (1‑25 mM; 24 h) increases cell viability and alleviates UVB‑triggered cytotoxicity in HaCaT keratinocytes^[1].
Indole‑3‑pyruvic acid (25 mM; 6 h) suppresses the secretion of pro‑inflammatory cytokines IL‑1β, IL‑6 and Cox‑2 in UVB‑irradiated HaCaT keratinocytes^[1].
Indole‑3‑pyruvic acid (5 mM; 1 h) attenuates p38 MAPK phosphorylation and down‑regulates Cox‑2 protein expression in UVB‑irradiated HaCaT keratinocytes^[1].
Indole‑3‑pyruvic acid (50‑250 μM; 24 h) activates aryl hydrocarbon receptor in HepG2 reporter cells^[2].
Indole‑3‑pyruvic acid (50 μM; 4 days) directly promotes type 1 regulatory T cell (Tr1) differentiation under Tr1‑polarizing cell culture conditions^[2].
In Vivo:Indole‑3‑pyruvic acid (100 mmol; topical application, two administrations) mitigates skin erythema, reduces dermal thickness, decreases transepithelial water loss, and inhibits the mRNA overexpression of IL‑1β, IL‑6 and Bax in the dorsal skin of UVB‑exposed HR‑1 hairless mice^[1].
Indole‑3‑pyruvic acid (0.1% diet; 5 days) up‑regulates colonic Cyp1a1 expression and activates intestinal AHR signalling pathway in BALB/c mice^[2].
Indole‑3‑pyruvic acid (0.1% diet; 2 weeks) increases the frequency of CD103⁺CD11b⁻ dendritic cells and decreases the proportion of CD103⁻CD11b⁺ dendritic cells in mesenteric lymph nodes of BALB/c mice^[2].
Indole‑3‑pyruvic acid (0.1% diet; 5 weeks) relieves diarrhoea and ameliorates colonic histopathological lesions in SCID mice with naive CD4⁺ T‑cell‑transfer‑induced colitis, reduces Th1‑related cytokine transcripts and elevates IL‑10 mRNA expression level in colon tissues of colitic SCID mice^[2].
Indole‑3‑pyruvic acid (100‑200 mg/kg; intraperitoneal injection, administered 1 h prior to behavioural test) increases the open‑arm entry ratio and open‑arm residence time, and antagonizes anxiogenic effects in the elevated‑plus‑maze mouse anxiety model^[2].