[CAS NO. 1416324-85-0] Cu-CPT22

Name: Cu-CPT22
Brand: Arctom Scientific
SKU: SLK-S8677

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1416324-85-0]

Store

Catalog

SLK-S8677

Brand

Selleck

CAS

1416324-85-0

DESCRIPTION [1416324-85-0]

Overview

MDL	MFCD26406409
Molecular Weight	362.37
Molecular Formula	C19H22O7
SMILES	O=C(C(C=C1O)=CC2=CC(OC)=C(O)C(O)=C2C1=O)OCCCCCC

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.7596 mL	13.7981 mL	27.5961 mL
5 mM	0.5519 mL	2.7596 mL	5.5192 mL
10 mM	0.2760 mL	1.3798 mL	2.7596 mL
50 mM	0.0552 mL	0.2760 mL	0.5519 mL

Description

CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).

Targets

TLR1/2 ^[1]
(Cell-free)

0.58 μM

In vitro

CU-CPT22 can compete with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with high inhibitory activity and specificity. The inhibition constant (Ki) is 0.41 ± 0.07 µM. CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells. It has no significant cytotoxicity at various concentrations up to 100 µM in RAW 264.7 cells using MTT assay. Kinase profiling shows that CU-CPT22 demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4). CU-CPT22 suppresses TLR1/2-mediated inflammation response. It inhibits about 60% of TNF-α and 95% of IL-1β at 8 µM in the RAW 264.7 cells.

In vivo

Cu-CPT22 administered before myocardial infarction (MI) significantly suppresses MI-induced upregulation of kidney injury molecule-1 (KIM-1), TLR2, TLR4, MyD88, and chemokine (C-C motif) ligand 2 levels and activation of NF-κB, whereas neutrophil gelatinase-associated lipocalin (NGAL) levels and IL-6 and TNF-α expression levels are unchanged.

References

[1] Cheng K, et al. Angew Chem Int Ed Engl. 2012, 51(49):12246-9.
[2] Ohno K, et al. Am J Physiol Heart Circ Physiol. 2017, 313(6):H1130-H1142.
[3] Bock S, et al. Pharmacol Res. 2016, 105:44-53