GNF 5837 | Alomone Labs G-145 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

GNF 5837

catalog :

G-145

more info or order :

Alomone Labs product webpage

image

image 1 :

Alomone Labs GNF 5837 inhibits BDNF induced ERK1/2 MAPK phosphorylation in TrkB stably expressed in HEK 293 cells. - Cells were serum deprived for 2 hrs followed by a 10 min stimulation with 10 ng/mlRecombinant human BDNF protein(#B-250) (lane 2) 10 and 100 MGNF 5837(#G-145) preincubated with 10 ng/ml Recombinant human BDNF protein for 10 min (lanes 3 and 4 respectively). Control cells incubated without Recombinant human BDNF protein are shown in lane 1. Cell proteins were resolved by SDS-PAGE and detected with anti-phospho-ERK1/2.

image 2 :

Peptide (C)EQREPKLNEKLHGR corresponding to amino acid residues 466-479 of rat NHE-3 (AccessionP26433). Intracellular C-terminus.

product information

CAT :

G-145

SKU :

G-145_10 mg

Product Name :

GNF 5837

Group Type :

Non Antibodies

Product Type :

S. Molecules

Storage After Reconstitution :

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Shipping and storage :

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

Product Page - Scientific background :

Three tropomyosin-related kinase (TrkA, TrkB, and TrkC) receptors bind the following neurotrophic factors with varied affinities: nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), neurotrophin-3 (NT-3), and neurotrophin-4 (NT-4); BDNF and NT-4 activate TrkB, while NGF and NT-3 activate TrkA and TrkC; NT-3 also activates the other two TRKs, albeit more weakly. After ligand binding, TRKs form dimers, and the subsequent kinase activation results in transphosphorylation of tyrosine residues which in turn enable the binding of cytoplasmic proteins that exhibit phosphotyrosine-binding (PTB) or Src-homology-2 (SH2) domains, such as phospholipase C (PLC-gamma1), p85 and Shc1-3.GNF-5837 is a novel oxindole urea inhibitor of TRKs. With exceptional binding affinity to TrkA, TrkB, and TrkC (IC50 = 0.011, 0.009, and 0.007 μM/L, respectively), GNF-5837 is a pan-TRK inhibitor that has enhanced selectivity for TRKs, and demonstrates efficiency in mammalian models of tumor. Many carcinomas - not necessarily nerve tissue-related - involve TRK signaling by NTs; GNF-5837 can therefore have useful application in cancer research in addition to other of its many other uses in many biological research branches4,5.

Supplier :

Alomone Labs

Target :

TrkA, TrkB, TrkC receptors

Long Description :

GNF 5837 (#G-145) is a highly pure, synthetic, and biologically active compound.

Short Description :

A Potent pan-Trk (Neurotrophin Receptor) Inhibitor

MW :

535.49

Source :

Synthetic

Molecular formula :

C28H21F4N5O2.

Effective Concentration :

1 nM - 10 µM.

Activity :

GNF 5837 displays antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively)1.

Reconstitution and Solubility :

40 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).

Solubility :

40 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).

Storage of solutions :

Up to four weeks at 4°C or three months at -20°C.

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Applications key :

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Purity :

>95%

CAS No :

1033769-28-6

Form :

Lyophilized powder.

Comment :

Contact Alomone Labs for technical support and product customization

UNSPSC :

41116134

Bioassay Tested :

Yes

Chemical Name :

(Z)-1-(3-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-ylamino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea.

more info or order :

Alomone Labs product webpage