2287331-29-5
Chemical Structure
TDI-6570
Synonym(s): TDI-006570
- CAS No.: 2287331-29-5
- Formula:C14H14ClFN2O2
- Molecular Weight:296.72
InChIKey: MLRXPYAADOGYND-UHFFFAOYSA-N
SMILES: O=C(CO)N1CC2=C(CC1)N(C)C3=C2C=CC(Cl)=C3F
Biological Activity: TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases[1][2][3].
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TDI-6570 | 99.64% | TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases. | ||||||||||||||||||||
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- [1]. Daisuke Tomita, et al. Inhibitors of cgas for treating autoinflammatory diseases and cancer metastasis. WO2020186027.
- [2]. Udeochu JC, et al. Tau activation of microglial cGAS-IFN reduces MEF2C-mediated cognitive resilience. Nat Neurosci. 2023;26(5):737-750. [Content Brief]
- [3]. Naguib S, et al. APOE3-R136S mutation confers resilience against tau pathology via cGAS-STING-IFN inhibition[J]. bioRxiv, 2025: 2024.04. 25.591140.
Keywords
