1258861-21-0
Chemical Structure
Taladegib hydrochloride
Synonym(s): LY2940680 hydrochloride
- CAS 番号: 1258861-21-0
- Formula:C26H25ClF4N6O
- Molecular Weight:548.96
InChIKey: ZULPZIIPOBSSNQ-UHFFFAOYSA-N
SMILES: CN1N=CC=C1C2=C3C(C=CC=C3)=C(N=N2)N4CCC(CC4)N(C)C(C5=C(C=C(C=C5)F)C(F)(F)F)=O.Cl
Biological Activity: Taladegib (LY2940680) hydrochloride is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC50 of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC50 of 7.6 nM in CGNP cell proliferation assays. Taladegib hydrochloride binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib hydrochloride can be used in studies of Hedgehog pathway-related cancers[1][2][3][4].
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Taladegib hydrochloride | Taladegib (LY2940680) hydrochloride is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC50 of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC50 of 7.6 nM in CGNP cell proliferation assays. Taladegib hydrochloride binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib hydrochloride can be used in studies of Hedgehog pathway-related cancers. | |||||||||||||||||||||
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- [1]. Ma W, et al. Reduced Smoothened level rescues Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. Journal of genetics and genomics = Yi chuan xue bao. 2018 May 20;45(5):237-246. [Content Brief]
- [2]. Fraveto A, et al. Sensitivity of Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents: A Study on Primary Cell Cultures. PloS one. 2015;10(11):e0142124. [Content Brief]
- [3]. Hoch L, et al. MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 2015 May;29(5):1817-29. [Content Brief]
- [4]. Lauressergues E, et al. Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model. Pharmacology research & perspectives. 2016 Apr;4(2):e00214. [Content Brief]
Keywords
