Image is an illustration, may not reflect the exact product sold.


Other products by Merck

Merck - 5.31091.0001 - Porcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem

  • MFR SKU: 5.31091.0001
  • ITEM #: 17954034
  • 0 Reviews / 0 Questions
$353.00
Stock Status: SHIPS SOON (reserve your unit today)
Average lead time for this brand: 2-3 weeks. Specific products may vary.

ITEM #: 17954034
A cell-permeable inhibitor of Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC from 50 pM to 1.1 nM).
This listing is for 5 mg Glass bottle

Merck - 5.31091.0001 - Porcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem

  • Item #: 17954034
  • MFR SKU: 5.31091.0001
  • Overview A cell-permeable C59 (Cat. No. 500496 ) structural analog that potently inhibits Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC 50 from 50 pM to 1.1 nM) via direct porcupine (Porcn), but not Wntless, affinity interaction. Shown to inhibit the proliferation of head and neck squamous cell carcinoma (HNSCC) line HN30 (IC 50 = 0.3 nM), but not 293T even at a high concentration of 20 µ M. In mice & rats receiving therapeutic LGK974 oral dosages (up to 5 mg/10 mL/kg/d), a delayed tissue Wnt signaling suppression (max inhibition 7 to 10 h post dosing) is seen due to pre-existing Wnt in tissue, followed by a full recovery of tissue Wnt signalling at 24 h upon drug clearance. The periodic daily inhibition/recovering cycle is shown to result in tumor regression in mice & rats, while allowing Wnt signaling-dependent normal tissue homeostasis. Overdosing is reported to result in loss of intestinal epithelium in rats receiving 14 consecutive 20 mg/kg daily oral dosages.
  • Catalogue Number 531091
  • Brand Family Calbiochem®
  • Synonyms 2-(2, 3-Dimethyl-2, 4-bipyridin-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide, Wnt Pathway Inhibitor XXIII, LGK-974
  • References Liu, J., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20224.
  • CAS number 1243244-14-5
  • Form Tan powder
  • Hill Formula CHNO
  • Chemical formula CHNO
  • Reversible Y
  • Quality Level MQ100
  • Primary Target Porcupine
  • Purity ≥ 97% by HPLC
  • Cell permeable Y
  • Ship Code Ambient Temperature Only
  • Toxicity Standard Handling
  • Storage +2° C to +8° C
  • Protect from Light Protect from light
  • Do not freeze Ok to freeze
  • Special Instructions Following reconstitution, aliquot and freeze (-20° C). Stock solutions are stable for up to 6 months at -20° C.
  • Packaged under inert gas Packaged under inert gas

There are no questions about this product yet. Be the first to ask a question.

0 out of 5 stars
5 Star
0 %
4 Star
0 %
3 Star
0 %
2 Star
0 %
1 Star
0 %

Review this product

Tell us about your personal experience

Recently Viewed Items