| Chemical Properties | Back Directory | [Boiling point ]
962.7±65.0 °C(Predicted) | [density ]
1.275±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
Soluble to 1 mg/ml in DMSO | [form ]
Solid | [pka]
3.93±0.19(Predicted) | [color ]
White to off-white | [InChIKey]
UCWNTWGHVCSMJP-AIPSELJTNA-N | [SMILES]
[C@@H](CC(C)C)(NC(=O)[C@@H](NC(=O)C)CC1C=CC=CC=1)C(=O)N[C@@H]([C@H](O)C)C(=O)N[C@@H](CC(=O)O)C(=O)CCl |&1:0,8,23,24,30,r| |
| Hazard Information | Back Directory | [Uses]
Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3[1]. | [Biological Activity]
Ac-FLTD-CMK is a selective gasdermin D (GSDMD) clevage inhibitor (IC50 = 46.7 nM329 nM1.49 μMrespectivelyagainst GSDMD clevage by human caspase-1-5-4 in cell-free enzymatic assays) th at suppresses pyroptosis downstream of both canonical and noncanonical inflammasomesas well as reduces IL-1β release following activation of the NLRP3 inflammasome in macrophages (10 μM 4h post 200 ng/mL LPS and 0.5h before ATP or nigericin). Ac-FLTD-CMK selectively blocks GSDMD clevage by inflammatory caspases without affecting apoptotic caspases (caspase-3 IC50 >100 μM) or apoptosis. | [IC 50]
Caspase-1: 46.7 nM (IC50); Caspase-4: 1.49 μM (IC50); Caspase-5: 329 nM (IC50); Caspase-11 | [storage]
Store at -20°C | [References]
[1] Jie Yang, et al. Mechanism of gasdermin D recognition by inflammatory caspases and their inhibition by a gasdermin D-derived peptide inhibitor. Proc Natl Acad Sci U S A. 2018 Jun 26;115(26):6792-6797. DOI:10.1073/pnas.1800562115 |
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