LYPLAL1-IN-1
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.34%
- CAS No.: 1966129-74-7
- Formula: C29H29N7O4
- Molecular Weight:539.59
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LYPLAL1-IN-1
More
Biological Activity
IC50: 0.006 μM (LYPLAL1-IN-1)[1]
LYPLAL1-IN-1 (30 min) showed potent inhibitory activity against human recombinant LYPLAL1 in in vitro enzyme inhibition assays, with an IC50 of 0.006 μM, and no significant inhibitory effect on CES1 (IC50 > 50 μM)[1].
LYPLAL1-IN-1 (compound 11) (10 μM, 20 μM; 24 h) increased cGAS palmitoylation levels in MDA-MB-231 cells, promoted HT-DNA-induced IRF3 phosphorylation, and at a concentration of 20 μM, enhanced cGAS dimerization and upregulated PD-L1 protein expression[2].
LYPLAL1-IN-1 (20 μM; 24 h) significantly increased the mRNA expression levels of IFNβ1 and CXCL10 in MDA-MB-231 cells, and this effect was dependent on cGAS[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1966129-74-7
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Appearance Solid
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Molecular Weight 539.59
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Formula C29H29N7O4
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Cell
Targeting LYPLAL1-mediated cGAS depalmitoylation enhances the response to anti-tumor immunotherapy. [Abstract]2023 Oct 5;83(19):3520-3532.e7. PMID: 37802025
Solvent & Solubility
DMSO : 2 mg/mL (3.71 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8533 mL | 9.2663 mL | 18.5326 mL | 46.3315 mL |
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