| Identification | Back Directory | [Name]
GNF-2 | [CAS]
778270-11-4 | [Synonyms]
GNF-2
CS-569
GNF2;GNF 2
GNF 2, >=98%
GNF-2 USP/EP/BP
Bcr-abl Inhibitor
Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem
3-(6-(4-(TRIFLUOROMETHOXY)PHENYLAMINO)PYRIMIDIN-4-YL)BENZAMIDE
3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
Benzamide, 3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-
3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide GNF-2
GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide | [EINECS(EC#)]
200-256-5 | [Molecular Formula]
C18H13F3N4O2 | [MDL Number]
MFCD09265253 | [MOL File]
778270-11-4.mol | [Molecular Weight]
374.32 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
H2O: <2mg/mL | [form ]
White solid | [color ]
off-white | [Water Solubility ]
H2O: <2mg/mL
DMSO: ≥5mg/mL | [InChI]
1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25) | [InChIKey]
WEVYNIUIFUYDGI-UHFFFAOYSA-N | [SMILES]
NC(=O)c1cccc(c1)-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2 |
| Hazard Information | Back Directory | [Description]
GNF-2 is an allosteric inhibitor of Bcr-Abl (IC50 = 267 nM).1 It is selective for Bcr-Abl over c-Abl and a panel of 63 additional kinases at 10 μM. It inhibits proliferation of Ba/F3 cells (IC50 = 138 nM). GNF-2 (10 μM) reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, via inhibition of IBV surface glycoprotein-induced syncytia formation and virus-cell fusion.2 It inhibits LPS-induced production of nitric oxide (NO) and TNF-α in BV-2 microglia when used at concentrations of 10 and 20 μM.3 GNF-2 (1 and 10 mg/kg) reduces paw edema and increases the latency to paw withdrawal in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA). It also decreases mechanical and thermal hyperalgesia in a mouse model of diabetic neuropathy induced by streptozotocin (STZ; Item No. 13104). | [Uses]
Bcr-abl Inhibitor is an inhibitor of c-Abl and Bcr-abl activity. It is a COVID19-related research product. | [Definition]
ChEBI: 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide is a member of pyrimidines. | [General Description]
A cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 μM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays. | [Biochem/physiol Actions]
GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC50 of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein. | [References]
[1] FRANCISCO J ADRIáN. Allosteric inhibitors of Bcr-abl–dependent cell proliferation[J]. Nature chemical biology, 2006, 2 2: 95-102. DOI: 10.1038/nchembio760
[2] JEANNE M SISK Carolyn E M Matthew B Frieman. Coronavirus S protein-induced fusion is blocked prior to hemifusion by Abl kinase inhibitors.[J]. Journal of General Virology, 2018, 99 5: 619-630. DOI: 10.1099/jgv.0.001047
[3] GYUN JEE SONG. A Bcr-Abl Inhibitor GNF-2 Attenuates Inflammatory Activation of Glia and Chronic Pain.[J]. Frontiers in Pharmacology, 2019: 543. DOI: 10.3389/fphar.2019.00543 |
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China Langchem Inc.
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