FM-381

Catalog No.S8541

For research use only.

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.

FM-381 Chemical Structure

CAS No. 2226521-65-7

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

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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 Research:

[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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 428.49
Formula

C24H24N6O2

CAS No. 2226521-65-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)C(=O)C(=CC1=CC=C(O1)C2=NC3=CN=C4C(=C3N2C5CCCCC5)C=CN4)C#N

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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