FM-381

SKU: orb1302099

Description

FM-381

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2226521-65-7
• MW: 428.49
• Purity: 99.33%
• Formula: C₂₄H₂₄N₆O₂
• SMILES: CN(C)C(=O)C(=C\c1ccc(o1)-c1nc2cnc3[nH]ccc3c2n1C1CCCCC1)\C#N
• Target: JAK
• Solubility: H2O:Insoluble;DMSO:12.5 mg/mL (29.17 mM)

Bioactivity

• Target IC50:
  JAK3:127 pM
• In Vitro:
  FM-381 is a potent covalent reversible inhibitor of JAK3 targetin the unique Cys909 a 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.
• Cell Research:
  CD4+ T Cell cytokine stimulation assay is performed. T cells are purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells are incubated for 1 hr with JAK inhibitors (FM381) (0, 10, 50, 100, 300 nM) or DMSO control and stimulated with cytokines for 30 min the cells are lysed, an the proteins are separated via PAGE and transferred to a polyvinylidene fluoride membrane the proteins of interest are blotted with specific antibodies and visualized with an infrared imaging syste.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, JAK, Janus kinase, JAK3, Inhibitor, FM381, FM-381, FM 381

Compound Identifiers

PubChem CID

122197584