Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 11,000 | |||
5 mg | 在庫あり | ¥ 26,000 | |||
10 mg | 在庫あり | ¥ 37,500 | |||
25 mg | 在庫あり | ¥ 78,000 | |||
50 mg | 在庫あり | ¥ 113,500 | |||
100 mg | 在庫あり | ¥ 166,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 29,000 |
説明 | FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. |
ターゲット&IC50 | JAK3:127 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]. |
細胞研究 | 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, and 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 system[1]. |
別名 | FM381 |
分子量 | 428.49 |
分子式 | C24H24N6O2 |
CAS No. | 2226521-65-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 12.5 mg/mL (29.17 mM)
You can also refer to dose conversion for different animals. 詳細
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FM-381 2226521-65-7 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK FM381 inhibit FM 381 Inhibitor Janus kinase inhibitor