FM-381

Catalog No.S8541 Batch:S854101

Technical Data

Formula	C₂₄H₂₄N₆O₂
Molecular Weight	428.49	CAS No.	2226521-65-7
Solubility (25°C)*	In vitro	DMSO	20 mg/mL (46.67 mM)
		Ethanol	2 mg/mL (4.66 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.)

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Biological Activity

Description

FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.

Targets

JAK3 ^[1]
(Cell-free)

127 pM

In vitro

FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper (GK) position +7 in JAK3 exhibited apparent JAK3 IC50 values of 0.127 nM, with 400-, 2700- and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. FM-381 was found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 shows an apparent EC50 of 100 nM in a dose dependent BRET assay and blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells up to 1 µM^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines CD4+ T Cell Concentrations 0, 10, 50, 100, 300 nM Incubation Time 1 h Method T cells were purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells were incubated for 1 hr with JAK inhibitors or DMSO control and stimulated with cytokines for 30 min. The cells were lysed, and the proteins were separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest were blotted with specific antibodies and visualized with an infrared imaging system.

Cell Assay:^{^[1]}

Cell lines
CD4+ T Cell
Concentrations
0, 10, 50, 100, 300 nM
Incubation Time
1 h
Method
T cells were purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells were incubated for 1 hr with JAK inhibitors or DMSO control and stimulated with cytokines for 30 min. The cells were lysed, and the proteins were separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest were blotted with specific antibodies and visualized with an infrared imaging system.

References

[1] Forster M, et al. Cell Chem Biol. 2016, 23(11):1335-1340.

Selleck's FM-381 has been cited by 1 publication

A homogeneous bioluminescent immunoassay to probe cellular signaling pathway regulation. [ Commun Biol, 2020, 3:8]	PubMed: 31909200

A homogeneous bioluminescent immunoassay to probe cellular signaling pathway regulation. [ Commun Biol, 2020, 3:8]

PubMed: 31909200

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SHIPPING AND STORAGE
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