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Ki16425

Catalog No. T6108 CAS 355025-24-0

Synonyms: Debio 0719

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively.

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Ki16425, CAS 355025-24-0

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Purity: 98%

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Description	Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively.
Targets&IC50	LPA3:0.93 μM(Ki), LPA1:0.34 μM(Ki), LPA2:6.5 μM(Ki)
In vitro	Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only a marginal effect in PC-12 cells and HL-60 cells, which means that Ki16425 seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. Ki16425 inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts. [1] Ki16425 reduces the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Ki16425 also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells. [2] Ki16425 markedly inhibits the expressions of COX-2 protein induced by synovial fluids. The enhancement of the IL-1 action by LPA on COX-2 expression is also inhibited by Ki16425. [3]
In vivo	Ki-16425 (30 mg/kg, i.p.) completely blocks LPA-induced neuropathic pain-like behaviors, when administered 30 min but not 90 min before lysophosphatidic acid injection, suggesting that Ki-16425 is a short-lived inhibitor. Ki-16425 also inhibits nerve injury-induced up-regulation of Caα2δ-1 in the dorsal root ganglion and reduction of SP immunoreactivity in the spinal dorsal horn. [4]
Kinase Assay	High-throughput screening: Screening is conducted at the ICCB-Longwood screening facility. 10 μL of recombinant USP14 protein are dispensed into each well of a 384-well low volume plate in duplicate, using a Wellmate plate dispenser. 33.3?nL of compound from the library are pin-transferred into the wells using a Seiko pin transfer robotic system, followed by pre-incubation for about 30?min. The last two columns of each plate are used for positive and negative controls for the assay. To initiate the enzyme reaction, 10?μL of VS-proteasome plus Ub-AMC mixture are added to each well, using a Wellmate dispenser. Samples are then incubated for another 45?min. Ub-AMC hydrolysis is measured at Ex355/Em460 using an Envision plate reader. The final concentrations of USP14, VS-proteasome and Ub-AMC are 15?nM, 1?nM and 0.8 μM, respectively. The final concentration of test compound is approximately 17?μM. Enzymes and substrates are prepared in Ub-AMC assay buffer (50?mM Tris-HCl (pH?7.5), 1?mM EDTA, 1?mM ATP, 5 mM MgCl2, 1?mM DTT, and 1 mg/Ml ovalbumin).

Synonyms	Debio 0719
Molecular Weight	474.96
Formula	C23H23ClN2O5S
CAS No.	355025-24-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 94 mg/mL (197.91 mM)

H2O: <1 mg/mL

Ethanol: 84 mg/mL(176.9 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Ohta H, et al, Mol Pharmacol, 2003, 64(4), 1994-12005. 2. Moughal NA, et al. J Neurochem, 2006, 98(6), 1920-1929. 3. Nochi H, et al. J Immunol, 2008, 181(7), 5111-5119. 4. Ma L, et al. J Neurochem, 2009, 109(2), 603-610.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Preclinical Compound Library GPCR Compound Library Inhibitor Library Anti-Cancer Active Compound Library Neuronal Signaling Compound Library Anti-Fibrosis Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

TAK-615 Tetradecyl Phosphonate ONO-7300243 Ki16198 TC LPA5 4 H2L5186303 GRI977143 DBIBB

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Keywords

Ki16425 355025-24-0 G蛋白偶联受体 LPA Receptor LPL Receptor Lysophospholipid Receptor Inhibitor Debio0719 Debio 0719 Ki-16425 inhibit Debio-0719 Ki 16425 inhibitor

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