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Purity: ≥98%
FM-381 (FM381) is a potent, specific, covalent reversible inhibitor of JAK3 with anti-inflammatory activity. It inhibits JAK with IC50 of 127 pM for JAK3, and is 410, 2700 and 3600-fold selective over JAK1, JAK2 and TYK2, respectively. FM-381 targets the unique Cys909 at the gatekeeper position +7 in JAK3. FM381 has no relevant effect on the activity of any tested kinases except JAK3 at a concentration of 100 nM. At 500 nM, FM381 moderately inhibits 11 other kinases besides JAK3 with residual activities below 50%. FM-381 is found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9).
| ln Vitro |
FM-381 is tested at 100 nM and 500 nM concentrations against a panel of 410 kinases. At 100 nM, FM-381 has no discernible impact on the activity of any of the examined kinases other than JAK3. Eleven additional kinases, including JAK3, are moderately inhibited by FM-381 at 500 nM, with residual activity less than 50%. A selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9) reveals that FM-381 is inactive. Human CD4+ T cells with specific JAK3 signaling inhibition from FM-381. In the dose-dependent BRET experiment, FM-381 exhibits an apparent EC50 of 100 nM. It also inhibits phosphorylation of STAT5 induced by IL2 (JAK3/JAK1 dependent) at 100 nM, but not JAK3 independent IL6 (JAK1/2/TYK dependent) stimulated STAT3 signaling in human CD4+ T cells up to 1 µM[1].
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| References |
[1]. Forster M, et al. Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. Cell Chem Biol. 2016 Nov 17;23(11):1335-1340
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| Molecular Formula |
C24H24N6O2
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| Molecular Weight |
428.49
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| CAS # |
2226521-65-7
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| SMILES |
CN(C(/C(C#N)=C/C1=CC=C(C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5)O1)=O)C
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3338 mL | 11.6689 mL | 23.3378 mL | |
| 5 mM | 0.4668 mL | 2.3338 mL | 4.6676 mL | |
| 10 mM | 0.2334 mL | 1.1669 mL | 2.3338 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Co-crystal Structures of JAK3 andCompounds4and5.Cell Chem Biol.2016 Nov 17;23(11):1335-1340. |
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 Induced Binding Pocket Around R911.Cell Chem Biol.2016 Nov 17;23(11):1335-1340. |
 Selective Inhibition of JAK3-Mediated Cytokine Signaling by Compounds4and5.Cell Chem Biol.2016 Nov 17;23(11):1335-1340. |
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