Stattic 19983-44-9

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Molecular Weight:

211.19 Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1.


Biological Activity


Stattic inhibits binding of a phosphotyrosine-containing peptide derived
from the gp130 receptor to the STAT3 SH2 domain in a strongly
temperature-dependent manner. Stattic only has a very weak effect on
binding of a tyrosinephosphorylated peptide to the SH2-domain of the
tyrosine kinase Lck. And it doesn`t inhibit dimerization of two other
dimeric transcription factors (c-Myc/Max and Jun/Jun). It also inhibits
fluorescein-labeled phosphopeptides to the SH2 domains of STAT1 and
STAT5b.


Stattic selectively inhibits DNA binding of STAT3 homodimers at a
concentration of 10 μM. Shown to inhibit cellular phosphorylation of
STAT3 at Tyr705 with little effect towards STAT1 phosphorylation at
Tyr701 (in HepG2 cells) or the phosphorylation of JAK1, JAK2, and c-Src
(in MDA-MB-231 and MDA-MB-235S cells). Stattic increases the apoptotic
rate of STAT3-dependent breast cancer cell lines.






Protocol(Only for Reference)


Kinase Assay: [1]

High-Throughput Screening and Fluorescence Polarization Assays

Screening is performed at approximately 30 °C. The specificity of screening hits is validated in analogous assays for binding of the test compounds to the SH2 domains of STAT1, STAT5, and Lck. The final concentration of buffer components used for all FP assays is 10 mM HEPES (pH 7.5), 1 mM EDTA, 0.1% Nonidet P-40, 50 mM NaCl, and 10% DMSO. The absence of dithiothreitol is essential for inhibitory activity. The sequences of the peptides are: STAT3, 5-carboxyfluorescein-GY(PO3H2)LPQTV-NH2; STAT1, 5-carboxyfluorescein-GY(PO3H2)DKPHVL; STAT5, 5-carboxyfluorescein-GY(PO3H2)LVLDKW; and Lck, 5-carboxyfluorescein-GY(PO3H2)EEIP. For specificity analysis at 30 °C, Proteins are used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37 °C, proteins are used at 370 nM (STAT3) or 100 nM (Lck). Proteins are incubated with test compounds in Eppendorf tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Before measurement at room temperature, the mixtures are allowed to equilibrate for at least 30 min. Test compounds are used at the indicated concentrations diluted from a 20× stock in DMSO. Binding curves and inhibition curves are fitted with SigmaPlot. All competition curves are repeated three times in independent experiment

Cell Assay: [2]

Cell lines	Ly3 cells
Concentrations	~2.5 μM
Incubation Time	48 h
Method	MTS

Animal Study: [2]

Animal Models	Ly3 parental NOD/SCID IL2R null xenograft
Formulation
Dosages	3.75 mg/kg every day
Administration	i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	211.19
Formula	C8H5NO4S
CAS No.	19983-44-9

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	42 mg/mL (198.87 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	Benzo[b]thiophene, 6-nitro-, 1,1-dioxide

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