SH-4-54

Names

[ Name ]:
SH-4-54

[Synonym ]:
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

Biological Activity

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.431±0.06 g/cm3

[ Boiling Point ]:
717.2±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₉H₂₇F₅N₂O₅S

[ Molecular Weight ]:
610.592

[ Flash Point ]:
387.5±35.7 °C

[ Exact Mass ]:
610.156067

[ PSA ]:
103.37000

[ LogP ]:
7.64

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.590

[ Storage condition ]:
-20℃

[ Water Solubility ]:
Insuluble (2.6E-5 g/L) (25 ºC)

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.