SH-4-54

Alias:
Cat No.:V1385 Purity: ≥98%
SH-4-54 (SH 454;SH4-54; SH454;SH-454) is anovel and potent STAT inhibitor with potential antineoplastic activity.
SH-4-54 Chemical Structure CAS No.: 1456632-40-8
Product category: STAT
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SH-4-54 (SH 454; SH4-54; SH454; SH-454) is a novel and potent STAT inhibitor with potential antineoplastic activity. It inhibits STAT3/5 with KD values of 300 nM and 464 nM, respectively. SH-4-54 shows potent anti-proliferative activity in vitro against glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nanomolar concentrations.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
At low nM concentrations, SH-4-54 efficiently inhibits STAT3 phosphorylation and its downstream transcriptional targets while also killing glioblastoma brain cancer stem cells (BTSCs). At therapeutic dosages, SH-4-54 effectively reduces pSTAT3 with nanomolar IC50s, blocking STAT3's downstream targets. It also exhibits no toxicity in human fetal astrocytes and demonstrates exceptional cytotoxicity in human BTSCs[1].
ln Vivo
In vivo, SH-4-54 inhibits pSTAT3 and demonstrates blood-brain barrier permeability, which together potently regulate the growth of glioma tumors. SH-4-54 reduces pSTAT3 expression in treated mice's tumor cells, highlighting the effectiveness of STAT3 inhibitors in treating BTSCs and confirming their therapeutic efficacy for use in GBM clinical applications. Treatable tumors seem to undergo more apoptosis and less proliferation when exposed to SH-4-54[1].
Animal Protocol
Suspended in 50% polyethylene glycol 300 in water; 10 mg/kg; i.p. injection
NOD-SCID bearing ed with BT73 glioma xenografts
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H27F5N2O5S
Molecular Weight
610.59
CAS #
1456632-40-8
SMILES
S(C1C(=C(C(=C(C=1F)F)F)F)F)(N(C([H])([H])[H])C([H])([H])C(N(C1C([H])=C([H])C(C(=O)O[H])=C([H])C=1[H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O)(=O)=O
InChi Key
VFPYGNNOSJWBHF-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H27F5N2O5S/c1-35(42(40,41)28-26(33)24(31)23(30)25(32)27(28)34)16-22(37)36(21-13-11-20(12-14-21)29(38)39)15-17-7-9-19(10-8-17)18-5-3-2-4-6-18/h7-14,18H,2-6,15-16H2,1H3,(H,38,39)
Chemical Name
4-(N-(4-cyclohexylbenzyl)-2-((2,3,4,5,6-pentafluoro-N-methylphenyl)sulfonamido)acetamido)benzoic acid
Synonyms

SH 454;SH-4-54;SH4-54; SH-454; SH 4-54; SH454.

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (163.8 mM)
Water:<1 mg/mL
Ethanol: 50 mg/mL(81.9 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6378 mL 8.1888 mL 16.3776 mL
5 mM 0.3276 mL 1.6378 mL 3.2755 mL
10 mM 0.1638 mL 0.8189 mL 1.6378 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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