1456632-40-8

1456632-40-8 structure

Name: SH-4-54
Chemical Name: Benzoic acid, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-
CAS Number: 1456632-40-8
Molecular Formula: C₂₉H₂₇F₅N₂O₅S
Molecular Weight: 610.592
Catalog: Biochemical Inhibitor Tyrosine protein kinase/signal transducer and transcriptional activator inhibitor (JAK/STAT) STAT inhibitor
Create Date: 2018-12-05 15:48:37
Modify Date: 2024-01-11 19:53:38
SH-4-54 is a most potent, small molecule, nonphosphorylated STAT inhibitor, with KDs of 300, 464 nM for STAT3 and STAT5, respectively.

Name	Benzoic acid, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-
Synonyms	4-[(4-Cyclohexylbenzyl){N-methyl-N-[(pentafluorophenyl)sulfonyl]glycyl}amino]benzoic acid Benzoic acid, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]- SH-4-54 4-[[(4-Cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]benzoic acid

Description	SH-4-54 is a most potent, small molecule, nonphosphorylated STAT inhibitor, with KDs of 300, 464 nM for STAT3 and STAT5, respectively.
Related Catalog	Signaling Pathways >> JAK/STAT Signaling >> STAT Signaling Pathways >> Stem Cell/Wnt >> STAT Research Areas >> Cancer
Target	STAT3:300 nM (Kd) STAT5:464 nM (Kd)
In Vitro	SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations.SH-4-54 shows unprecedented cytotoxicity in human BTSCs, displays no toxicity in human fetal astrocytes, potently suppresses pSTAT3 with nanomolar IC50s, inhibiting STAT3's downstream targets, and shows no discernible off-target effects at therapeutic doses[1].
In Vivo	SH-4-54 exhibits blood-brain barrier permeability potently controls glioma tumor growth, and inhibits pSTAT3 in vivo. SH-4-54 demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.SH-4-54 decreases pSTAT3 expression in tumor cells of treated mice. SH-4-54 appears to decrease proliferation and increase apoptosis of treated tumors[1].
References	[1]. Haftchenary S, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett. 2013 Sep 8;4(11):1102-1107.