SBI-477

Catalog No.S3187 Batch:S318702

Technical Data

Formula	C₂₄H₂₅N₃O₆S
Molecular Weight	483.54	CAS No.	781628-99-7
Solubility (25°C)*	In vitro	DMSO	97 mg/mL (200.6 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

SBI-477 is an insulin signaling inhibitor that deactivates the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain-containing 4 (ARRDC4). SBI-477 inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.

Targets

MondoA ^[1]

TXNIP ^[1]

ARRDC4 ^[1]

TAG ^[1]

In vitro

SBI-477, that coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes, stimulates insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain containing 4 (ARRDC4).^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Primary human skeletal myotubes Concentrations -- Incubation Time 24 h Method Primary human skeletal myotubes were grown and differentiated in 24-well plates. Cells were treated with the indicated concentration of SBI-477 for 24 h. Following compound treatment, cells were rinsed three times with PBS and then incubated in 125μM [<sup>3</sup>H]-palmitic acid (60 Ci/mmol) bound to fatty acid free albumin containing 1mM carnitine for 2 hours at 37℃. The cell medium was transferred to a tube containing cold 10% trichloroacetic acid (TCA). The tubes were centrifuged at 8,500 x g for 10 minutes at 4℃. The supernatant was immediately removed, mixed with 6N NaOH, and applied to ion-exchange resin. The eluate was collected, measured by liquid scintillation analyzer and normalized to total protein amount. The amount of cell protein was measured.

Cell Assay:^{^[1]}

Cell lines
Primary human skeletal myotubes
Concentrations
--
Incubation Time
24 h
Method
Primary human skeletal myotubes were grown and differentiated in 24-well plates. Cells were treated with the indicated concentration of SBI-477 for 24 h. Following compound treatment, cells were rinsed three times with PBS and then incubated in 125μM [<sup>3</sup>H]-palmitic acid (60 Ci/mmol) bound to fatty acid free albumin containing 1mM carnitine for 2 hours at 37℃. The cell medium was transferred to a tube containing cold 10% trichloroacetic acid (TCA). The tubes were centrifuged at 8,500 x g for 10 minutes at 4℃. The supernatant was immediately removed, mixed with 6N NaOH, and applied to ion-exchange resin. The eluate was collected, measured by liquid scintillation analyzer and normalized to total protein amount. The amount of cell protein was measured.

References

[1] Byungyong Ahn, et al. J Clin Invest. 2016 Sep 1;126(9):3567-79.

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