MYF-01-37

Catalog No.S8950 Batch:S895002

Technical Data

Formula	C₁₅H₁₇F₃N₂O
Molecular Weight	298.3	CAS No.	2416417-65-5
Solubility (25°C)*	In vitro	DMSO	60 mg/mL (201.13 mM)
		Ethanol	60 mg/mL (201.13 mM)
		Water	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

MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein.

Targets

TEAD ^[1]

In vitro

MYF-01-37 is developed as a covalent binder to TEAD, targeting Cys380 when incubated with the TEAD2 protein (C359 in TEAD1). Pretreating cells with MYF-01-37 leads to loss of direct TEAD pull-down by biotin-MYF-01-037 from whole-cell lysate, confirming MYF-01-037 binding to TEAD in cells.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines PC9 cells Concentrations 10 μM, 1 μM Incubation Time 6 h Method Cells are treated with test compounds for 6 h at the indicated doses. Total cell lysates are prepared using pulldown buffer. To pull down TEADs, 1 mg of total protein is combined with biotinylated MYF-01-37 at 1 μM and rotated at 4 ℃ for 6 hrs followed by RT for 1 h. Subsequently, streptavidin agarose resin (30 ml 50% slurry) is added and samples rotated for another 2 h at 4 ℃. The resin is subsequently washed 3× with pulldown buffer, and TEADs released from the resin by boiling for 10 min in 2× gel loading buffer and resolved by western blotting. As a loading control, 25 mg of total protein is used.

Cell Assay:^{^[1]}

Cell lines
PC9 cells
Concentrations
10 μM, 1 μM
Incubation Time
6 h
Method
Cells are treated with test compounds for 6 h at the indicated doses. Total cell lysates are prepared using pulldown buffer. To pull down TEADs, 1 mg of total protein is combined with biotinylated MYF-01-37 at 1 μM and rotated at 4 ℃ for 6 hrs followed by RT for 1 h. Subsequently, streptavidin agarose resin (30 ml 50% slurry) is added and samples rotated for another 2 h at 4 ℃. The resin is subsequently washed 3× with pulldown buffer, and TEADs released from the resin by boiling for 10 min in 2× gel loading buffer and resolved by western blotting. As a loading control, 25 mg of total protein is used.

References

[1] Kari J Kurppa, et al. Cancer Cell. 2020 Jan 13;37(1):104-122.e12.

Selleck's MYF-01-37 has been cited by 1 publication

Targeting the Hippo/YAP/TAZ signalling pathway: Novel opportunities for therapeutic interventions into skin cancers [ Exp Dermatol, 2022, 31(10):1477-1499]	PubMed: 35913427

Targeting the Hippo/YAP/TAZ signalling pathway: Novel opportunities for therapeutic interventions into skin cancers [ Exp Dermatol, 2022, 31(10):1477-1499]

PubMed: 35913427

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SHIPPING AND STORAGE
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