614305
TLR1/TLR2 Antagonist
Synonym(s):
3,4,6-trihydroxy-2-methoxy-5-oxo-5H-benzocycloheptene-8-carboxylic acid, 6-trihydroxy-2-methoxy-5-oxo-5H-benzocycloheptene-8-carboxylic acid, TLR1/TLR2 Antagonist, hexyl ester
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About This Item
Linear Formula:
C19H22O7
NACRES:
NA.51
UNSPSC Code:
51111800
Form:
(Orange solid)
Storage condition:
OK to freeze
form
(Orange solid)
storage condition
OK to freeze
solubility
soluble (DMSO (100 mg/ml). Use only fresh DMSO for reconstitution.)
storage temp.
2-8°C
General description
A cell-permeable benzotropolone compound that selectively antagonizes agonist-dependent TLR1/TLR2 heterodimer activation (IC50 = 580 nM against Pam3CSK4- (Cat. No. 506350) stimulated NO production in RAW264.7) by competing for TLR1/TLR2 binding (Ki = 410 nM against Pam3CSK4 in competition binding assays), displaying no cytotoxicity in RAW264.7 cultures (100 µM for 24 h) and exhibiting little inhibitory activity against a panel of 10 kinases (by <11% at 5 µM) or agonist-dependent activation of other TLRs (0% inhibition of TLR2/TLR6, TLR3, TLR4, TLR7 activation at 0.5 µM). Computer-aided in silico structural analysis reveals that the highly TLR1/TLR2-over-TLR2/TLR6 selective nature of CU-CPT22 is due to the exclusive location of CU-CPT22 R6 hexyl ester and Pam3CSK4 amide-linked N-pamitoyl fatty acid side chain competition site in TLR1, but not in TLR6.
signalword
Danger
hcodes
Hazard Classifications
Aquatic Acute 1 - Aquatic Chronic 1 - Resp. Sens. 1
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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