CY-09

CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.

Product information

CAS Number: 1073612-91-5

Molecular Weight: 423.43

Formula: C19H12F3NO3S2

Chemical Name: 4-{[(5Z)-4-oxo-2-sulfanylidene-3-{[3-(trifluoromethyl)phenyl]methyl}-1,3-thiazolidin-5-ylidene]methyl}benzoic acid

Smiles: OC(=O)C1C=CC(/C=C2\SC(=S)N(CC3C=C(C=CC=3)C(F)(F)F)C\2=O)=CC=1

InChiKey: DJTINRHPPGAPLD-DHDCSXOGSA-N

InChi: InChI=1S/C19H12F3NO3S2/c20-19(21,22)14-3-1-2-12(8-14)10-23-16(24)15(28-18(23)27)9-11-4-6-13(7-5-11)17(25)26/h1-9H,10H2,(H,25,26)/b15-9-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 150 mg/mL (354.25 mM). H2O : < 0.1 mg/mL (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

CY-09 exhibits a dose-dependent inhibitory effect on monosodium urate (MSU), nigericin, ATP-induced caspase-1 activation and IL-1β secretion at the doses of 1 to10 µM in LPS-primed bone marrow-derived macrophages (BMDMs). Cytosolic LPS-induced noncanonical NLRP3 activation in BMDMs can also be blocked by CY-09 treatment. CY-09 specifically inhibits NLRP3 inflammasome activation and has no effect on LPS-induced priming effects. CY-09 treatment remarkably suppresses nigericin-induced ASC oligomerization. It is found that CY-09 treatment inhibits the interaction of Flag-NLRP3 and mCherry-NLRP3 in HEK-293T cells, suggesting that CY-09 blocks NLRP3 oligomerization.

In Vivo:

CY-09 treatment in vivo efficiently suppresses monosodium urate (MSU) injection-induced IL-1β production and neutrophil influx, suggesting that CY-09 can block MSU-induced NLRP3 inflammasome activation in vivo. CY-09 treatment also increases the survival of NLRP3 mutant mice up to days 30 to 48 even after treatment is stopped at day 25. The caspase-1 cleavage observed in adipose tissue of high-fat diet (HFD)-treated mice is also suppressed by CY-09.

References:

1. Jiang H, et al. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238.

Products are for research use only. Not for human use.