受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H24N6O2 |
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分子量 | 428.49 | CAS No. | 2226521-65-7 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | 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. |
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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]. |
細胞アッセイ | 細胞株 | CD4+ T Cell |
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濃度 | 0, 10, 50, 100, 300 nM | |
反応時間 | 1 h | |
実験の流れ | 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. |
A homogeneous bioluminescent immunoassay to probe cellular signaling pathway regulation. [ Commun Biol, 2020, 3:8] | PubMed: 31909200 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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