Ki16425_product_DataBase

Bioactivity

Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK[1][2]. Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells[3].

Target

Ki: 0.34 μM (LPA1), 0.93 μM (LPA3), 6.5 μM (LPA2)

Invitro

Ki16425 (10 μM; 1.5 hours; HEK293A cells) treatment blocks LPA-induced dephosphorylation of YAP/TAZ in HEK293A cells. Ki16425 partially inhibits the ability of serum to repress YAP/TAZ phosphorylation, particularly at low serum concentrations (0.2%)[3]. Western Blot Analysis[3] Cell Line:

In Vivo

Ki16425 (Debio 0719) (1-30 mg/kg; i.p.; at 30 min prior to LPA injection) inhibits LPA-induced neuropathic pain-like behaviors[4]. Animal Model:

Name

Ki16425

CAS

355025-24-0

Formula

C23H23ClN2O5S

Molar Mass

474.96

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Ohta H, et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.Mol Pharmacol, 2003, 64(4), 994-1005. [2]. Moughal NA, et al. Protean agonism of the lysophosphatidic acid receptor-1 with Ki16425 reduces nerve growth factor-induced neurite outgrowth in pheochromocytoma 12 cells. J Neurochem, 2006, 98(6), 1920-1929. [3]. Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012 Aug 17;150(4):780-91. [4]. Ma L, et al. Evidence for lysophosphatidic acid 1 receptor signaling in the early phase of neuropathic pain mechanisms in experiments using Ki-16425, a lysophosphatidic acid 1 receptor antagonist. J Neurochem, 2009, 109(2), 603-610.

PeptideDB

Ki16425

CAS: 355025-24-0 F: C23H23ClN2O5S W: 474.96