1966129-74-7
Chemical Structure
LYPLAL1-IN-1
- CAS No.: 1966129-74-7
- Formula:C29H29N7O4
- Molecular Weight:539.59
IUPAC Name: (2R,3R)-1-(3-(4-(2-morpholinopyrimidin-5-yl)phenyl)-1H-1,2,4-triazole-1-carbonyl)-2-phenylpiperidine-3-carboxylic acid
InChIKey: OWBNMAVVNDAXQY-RPBOFIJWSA-N
SMILES: O=C([C@H]1[C@H](C2=CC=CC=C2)N(C(N3N=C(C4=CC=C(C5=CN=C(N6CCOCC6)N=C5)C=C4)N=C3)=O)CCC1)O
Biological Activity: LYPLAL1-IN-1 (compound 11) is a selective, covalent, and irreversible inhibitor of the lysophospholipase-like enzyme LYPLAL1 (IC50 = 6 nM). LYPLAL1-IN-1 shows selectivity against other serine hydrolases such as carboxylesterase CES1 (IC50 > 50 μM for CES1). LYPLAL1-IN-1 inhibits the depalmitoylation function of LYPLAL1, blocking its depalmitoylation modification of cyclic GMP-AMP synthase (cGAS), thereby promoting cGAS dimerization and activation, and initiating the cGAS-STING pathway-mediated innate immune response. LYPLAL1-IN-1 can enhance DNA-induced type I interferon production, upregulate PD-L1 expression in tumor cells, and promote the accumulation of tumor-infiltrating CD8+ T cells, with the core function of strengthening the anti-tumor immune response. LYPLAL1-IN-1 is primarily used in tumor immunology research, especially in combination with PD-1/PD-L1 inhibitors[1][2].
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LYPLAL1-IN-1 | 99.34% | LYPLAL1-IN-1 (compound 11) is a selective, covalent, and irreversible inhibitor of the lysophospholipase-like enzyme LYPLAL1 (IC50 = 6 nM). LYPLAL1-IN-1 shows selectivity against other serine hydrolases such as carboxylesterase CES1 (IC50 > 50 μM for CES1). LYPLAL1-IN-1 inhibits the depalmitoylation function of LYPLAL1, blocking its depalmitoylation modification of cyclic GMP-AMP synthase (cGAS), thereby promoting cGAS dimerization and activation, and initiating the cGAS-STING pathway-mediated innate immune response. LYPLAL1-IN-1 can enhance DNA-induced type I interferon production, upregulate PD-L1 expression in tumor cells, and promote the accumulation of tumor-infiltrating CD8+ T cells, with the core function of strengthening the anti-tumor immune response. LYPLAL1-IN-1 is primarily used in tumor immunology research, especially in combination with PD-1/PD-L1 inhibitors. | ||||||||||||||||||||
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References
- [1]. Ahn K, et al. Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism. ACS Chem Biol. 2016 Sep 16;11(9):2529-40. [Content Brief]
- [2]. Fan Y, et al. Targeting LYPLAL1-mediated cGAS depalmitoylation enhances the response to anti-tumor immunotherapy. Mol Cell. 2023 Oct 5;83(19):3520-3532.e7. [Content Brief]
