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Wnt&Beta catenin

LGK974 (1243244-14-5)

LGK-974, purity > 98%, is in stock. The same day shipping out after order is received. Note: Lead time for order of > 1g is about 6 weeks

Not Intended for Therapeutic Use. For research use only.

CAS: 1243244-14-5 Category

LGK974 (1243244-14-5) Description

LGK974, aslo known as is a selective and orally bioavailable Porcupine (PORCN) inhibitor under development for the treatment of cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner. WNT974 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational acylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine, a membrane-bound O-acyltransferase (MBOAT), is required for the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion and activity. Wnt signaling is dysregulated in a variety of cancers.

 

LGK974 (1243244-14-5) Specifications

Product Name LGK974
Synonym  LGK974; LGK-974; LGK 974; WNT974; WNT 974; WNT-974.
Chemical Name 2-(2′,3-dimethyl-[2,4′-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Drug Class N/A
Purity ≥ >98%
CAS Number  1243244-14-5
Molecular Formula  C23H20N6O
Molecular Weight 396.44
Monoisotopic Mass 396.16986
MDL number SML0795
InChIKey XXYGTCZJJLTAGH-UHFFFAOYSA-N
InChi Code  InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
SMILES   O=C(NC1=NC=C(C2=NC=CN=C2)C=C1)CC3=CN=C(C4=CC(C)=NC=C4)C(C)=C3
Form  PF670462
Color white
Solubility  Soluble in DMSO
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life > >5 years if stored properly
Handling SDS
Application In preparation of a product treating polycystic kidney disease is disclosed

 


=

RIDADR NONH for all modes of transport

References:

[1]. Guimaraes PPG, Tan M, Tammela T, Wu K, Chung A, Oberli M, Wang K, Spektor R, Riley RS, Viana CTR, Jacks T, Langer R, Mitchell MJ. J Control Release. 2018 Nov 28;290:75-87. doi: 10.1016/j.jconrel.2018.09.025. Epub 2018 Oct 2.

[2]. Yang JM, Huang HM, Cheng JJ, Huang CL, Lee YC, Chiou CT, Huang HT, Huang NK, Yang YC. Toxicology. 2018 Dec 1;410:65-72. doi: 10.1016/j.tox.2018.09.003. Epub 2018 Sep 8.

[3]. Suwala AK, Koch K, Rios DH, Aretz P, Uhlmann C, Ogorek I, Felsberg J, Reifenberger G, Köhrer K, Deenen R, Steiger HJ, Kahlert UD, Maciaczyk J. Oncotarget. 2018 Apr 27;9(32):22703-22716. doi: 10.18632/oncotarget.25210. eCollection 2018 Apr 27.

[4].Madan B, McDonald MJ, Foxa GE, Diegel CR, Williams BO, Virshup DM. Bone Res. 2018 May 25;6:17. doi: 10.1038/s41413-018-0017-8. eCollection 2018.

[5]. Funck-Brentano T, Nilsson KH, Brommage R, Henning P, Lerner UH, Koskela A, Tuukkanen J, Cohen-Solal M, Movérare-Skrtic S, Ohlsson C. J Endocrinol. 2018 Jul;238(1):13-23. doi: 10.1530/JOE-18-0153. Epub 2018 May 2.

1 review for LGK974 (1243244-14-5)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The LGK974 (1243244-14-5) is high purity,also customer service is pretty nice !gotta try!!

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