≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
FM-381 is aJAK3specific 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.
Targets
JAK3 (Cell-free) 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.
Cell Research(from reference)
Cell lines：CD4+ T Cell
Concentrations：0, 10, 50, 100, 300 nM
Incubation Time：1 h
| ALogP | 4.084 |
|---|---|
| hba_count | 4 |
| HBD Count | 1 |
| Rotatable Bond | 4 |
| Pubchem Sid | 504772965 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504772965 |
| Canonical Smiles | CN(C)C(=O)C(=CC1=CC=C(O1)C2=NC3=CN=C4C(=C3N2C5CCCCC5)C=CN4)C#N |
| IUPAC Name | (E)-2-cyano-3-[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]-N,N-dimethylprop-2-enamide |
| InChIKey | GJMZWYLOARVASY-NTCAYCPXSA-N |
| INCHI | 1S/C24H24N6O2/c1-29(2)24(31)15(13-25)12-17-8-9-20(32-17)23-28-19-14-27-22-18(10-11-26-22)21(19)30(23)16-6-4-3-5-7-16/h8-12,14,16H,3-7H2,1-2H3,(H,26,27)/b15-12+ |
| Isomeric SMILES | CN(C)C(=O)/C(=C/C1=CC=C(O1)C2=NC3=CN=C4C(=C3N2C5CCCCC5)C=CN4)/C#N |
| Molecular Weight | 428.49 |
| Reaxy-Rn | 30342556 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=30342556&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Class | Pyrrolopyridines |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Pyrrolopyridines |
| Alternative Parents | Imidazo-[4,5-c]pyridines Pyridines and derivatives N-substituted imidazoles Tertiary carboxylic acid amides Pyrroles Heteroaromatic compounds Furans Oxacyclic compounds Nitriles Azacyclic compounds Organopnictogen compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Imidazo-[4,5-c]pyridine - Pyrrolopyridine - Imidazopyridine - Pyridine - N-substituted imidazole - Heteroaromatic compound - Tertiary carboxylic acid amide - Pyrrole - Imidazole - Furan - Azole - Carboxamide group - Oxacycle - Azacycle - Nitrile - Carbonitrile - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Carbonyl group - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as pyrrolopyridines. These are compounds containing a pyrrolopyridine moiety, which consists of a pyrrole ring fused to a pyridine. Pyrrole is 5-membered ring consisting of four carbon atoms and one nitrogen atom. Pyridine is a 6-membered ring consisting of five carbon atoms and one nitrogen center. |
| External Descriptors | Not available |
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Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
 C23081486 | Certificate of Analysis | Dec 05, 2024 | F414048 |
| C23081492 | Certificate of Analysis | Dec 05, 2024 | F414048 |
| C23081493 | Certificate of Analysis | Dec 05, 2024 | F414048 |
| C23081495 | Certificate of Analysis | Dec 05, 2024 | F414048 |
| C23081501 | Certificate of Analysis | Dec 05, 2024 | F414048 |
| Solubility | Solubility (25°C) In vitro DMSO: 20 mg/mL (46.67 mM); Ethanol: 2 mg/mL (4.66 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 20 |
| DMSO(mM) Max Solubility | 46.67553502 |
| Water(mg / mL) Max Solubility | ＜1 |
| Molecular Weight | 428.500 g/mol |
| XLogP3 | 3.200 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 4 |
| Exact Mass | 428.196 Da |
| Monoisotopic Mass | 428.196 Da |
| Topological Polar Surface Area | 104.000 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 785.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 1 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 1 |
| Covalently-Bonded Unit Count | 1 |
