| Identification | Back Directory | [Name]
JAK3-IN-6 | [CAS]
1443235-95-7 | [Synonyms]
JAK3-IN-6
JAK3-IN-2
JAK3 inhibitor 6
JAK3-IN-6 (Compound 2)
SelectiveJAK3inhibitor1
JAK3-IN-2
(JAK3 inhibitor 2)
ethyl 4-{3-[(2-methylacryloyl)amino]phenyl}-7H-pyrrolo[2,3-d]pyrimidine-5-carboxylate
7H-Pyrrolo[2,3-d]pyrimidine-5-carboxylic acid, 4-[3-[(2-methyl-1-oxo-2-propen-1-yl)amino]phenyl]-, ethyl ester | [Molecular Formula]
C19H18N4O3 | [MDL Number]
MFCD31692331 | [MOL File]
1443235-95-7.mol | [Molecular Weight]
350.37 |
| Chemical Properties | Back Directory | [density ]
1.302±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: 260 mg/mL (742.07 mM) | [form ]
Solid | [pka]
10.26±0.50(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM. | [Biological Activity]
JAK3-IN-6 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM and 740 nM for JAK3, JAK1 and JAK2, respectively. It is more selective for JAK3 than BMX, EGFR, ITK and BTK. | [in vitro]
JAK3-IN-6 is a potent JAK3 inhibitor with IC50 of 0.15 nM, with 4300-fold selectivity for JAK3 over JAK1 in enzymatic activity assays, erythropoietin and 67-fold and 140-fold higher selectivity for granulocyte-macrophage colony-stimulating factor. | [in vivo]
JAK3-IN-6 completely inhibits the progression of inflammatory responses. | [target]
| Target | Value | JAK3
(Cell-free assay) | 0.07 nM(Ki) | JAK1
(Cell-free assay) | 320 nM(Ki) | JAK2
(Cell-free assay) | 740 nM(Ki) |
| [IC 50]
JAK3: 0.15 nM (IC50) | [storage]
Store at -20°C | [References]
[1] ARYL SULFONOHYDRAZIDES. WO2017027400A1.
[2] Elwood F, et al. Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor. J Pharmacol Exp Ther. 2017 May;361(2):229-244. DOI:10.1124/jpet.116.239723 |
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