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5.09105

Sigma-Aldrich

STAT3/STAT5 Dual Inhibitor, SH-4-54

Synonym(s):

STAT3/STAT5 Dual Inhibitor, SH-4-54, SH-04-54, SH0454, SH454, 4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)benzoic acid, STAT3 Inhibitor XIX, STAT5 Inhibitor IV

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About This Item

Empirical Formula (Hill Notation):
C29H27F5N2O5S
CAS Number:
Molecular Weight:
610.59
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥94% (HPLC)

Quality Level

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

General description

A cell-permeable BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity and is 4-fold more potent in competing against phosphopeptide for binding SH2 domain of STAT3 over STAT1, exhibiting little potency against upstream kinases or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) in cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice and effectively inhibit BT73 glioma proliferation in xenografted murine brain (10 mg/kg/d via i.p.; 4 d on/ 3 d off) in vivo.
A cell-permeable, salicyclic-to-benzoic acid-substituted BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity (koff/kon = KD = 300 and 464 nM, respectively) and is 4-fold more potent in competing against phosphopeptide for binding to SH2 domain of STAT3 over STAT1 (Ki = 23.5 and 92.3 µM, respectively; [phosphopeptide] = 10 nM), exhibiting little potency against the kinase activity of upstream kinases (Akt1, Erk1, JAK1/2, c-Src) or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice (Conc in brain = 313 nM 30 min post 10 mg/kg i.p. dosing) and effectively inhibit BT73 glioma proliferation in xenografted murine brain via apoptosis induction (10 doses: 10 mg/kg i.p., 4 d on/ 3 d off) in vivo.

Biochem/physiol Actions

Cell permeable: yes
Reversible: yes
Secondary Target
STAT5

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Haftchenary, S., et al. 2013. ACS Med. Chem. Lett.4, In press.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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