504433-23-2

504433-23-2 structure

Name: GW441756
Chemical Name: 1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-one
CAS Number: 504433-23-2
Molecular Formula: C₁₇H₁₃N₃O
Molecular Weight: 275.305
Catalog: Biochemical Inhibitor Protein tyrosine kinase
Create Date: 2018-12-29 08:46:31
Modify Date: 2024-01-02 08:26:20
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.IC50 Value: 2 nM [1]Target: TrkAin vitro: GW441756 specifically blocked TrkA-induced cell death in a dose-dependent manner, but there was no effect in uninduced cells. TrkA ability to induce γH2AX production was significantly downregulated by both K-252a and GW441756 in the absence of DNA damage inducer. In addition, it was also suppressed by K-252a during DNA damage by doxorubicin treatment, but not by GW441756 [2].

Name	1,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-2H-pyrrolo[3,2-b]pyridin-2-one
Synonyms	(3E)-3-[(1-Methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one 2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-, (3Z)- (3Z)-3-[(1-Methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one 2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-, (3E)- (3Z)-3-[(1-methyl-1H-indol-3-yl)methylidene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one GW 441756 GW441756

Description	GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.IC50 Value: 2 nM [1]Target: TrkAin vitro: GW441756 specifically blocked TrkA-induced cell death in a dose-dependent manner, but there was no effect in uninduced cells. TrkA ability to induce γH2AX production was significantly downregulated by both K-252a and GW441756 in the absence of DNA damage inducer. In addition, it was also suppressed by K-252a during DNA damage by doxorubicin treatment, but not by GW441756 [2].
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor Research Areas >> Cancer
References	[1]. Wood ER, Kuyper L, Petrov KG, Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7. [2]. Eun Joo Jung, Choong Won Kim, Deok Ryong Kim. Cytosolic accumulation of γH2AX is associated with tropomyosin-related kinase A-induced cell death in U2OS cells. Exp Mol Med. 2008 June 30; 40(3): 276-285.