769856-81-7
Chemical Structure
TPT-260
Synonym(s): TPU260
- CAS No.: 769856-81-7
- Formula:C8H12N4S3
- Molecular Weight:260.40
IUPAC Name: thiophene-2,5-diylbis(methylene) dicarbamimidothioate
InChIKey: XGDUNTSTRCLVLN-UHFFFAOYSA-N
SMILES: NC(SCC1=CC=C(CSC(N)=N)S1)=N
Biological Activity: TPT-260 (TPU260), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease[1][2][3][4].
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TPT-260 | TPT-260 (TPU260), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease. | |||||||||||||||||||||
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- [1]. Zhao J, et al. Loss of VMP1 Impairs Tight Junction Recycling and Aggravates Intestinal Barrier Dysfunction in Inflammatory Bowel Disease. Adv Sci (Weinh). Published online February 27, 2026. [Content Brief]
- [2]. Qian J, et al. Therapeutic Potential of TPT-260 in Ischemic Stroke: An Investigation Into Its Anti-Inflammatory Effects and Impact on Microglial Activation. J Inflamm Res. 2025 Mar 1;18:3055-3066. [Content Brief]
- [3]. Singh V, et al. Cholera toxin inhibits SNX27-retromer-mediated delivery of cargo proteins to the plasma membrane. J Cell Sci. 2018;131(16):jcs218610. Published 2018 Aug 17. [Content Brief]
- [4]. Mecozzi VJ, et al. Pharmacological chaperones stabilize retromer to limit APP processing. Nat Chem Biol. 2014 Jun;10(6):443-9. [Content Brief]
Keywords
