FM-381 NEW
| Price | $48 | $113 | $163 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: FM-381 | CAS No.: 2226521-65-7 |
| Purity: 99.33% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | FM-381 |
| Description | 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. |
| 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, 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]. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : Insoluble DMSO : 12.5 mg/mL (29.17 mM) |
| Keywords | FM-381 | inhibit | JAK | FM 381 | Inhibitor | Janus kinase |
| Inhibitors Related | Delgocitinib | Deucravacitinib | Fedratinib | RO8191 | Ruxolitinib | Tofacitinib Citrate | CEP-33779 | Ruxolitinib phosphate | JAK-IN-10 | Baricitinib | Tofacitinib | Ritlecitinib |
| Related Compound Libraries | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | JAK-STAT Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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