Our laboratory has not validated this product for use on human JAK. However, based on the provided citation, the inhibitor appears to demonstrate effective activity on human cells as well. The study titled "Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor" published in Int J Oncol. 2018 Oct;53(4):1681-1690 (PMID: 30066853) supports this observation.
420097
JAK Inhibitor I
InSolution, ≥98%
Sinónimos:
InSolution JAK Inhibitor I, 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, P6, Pyridone 6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
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500 μG
203,00 €
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About This Item
Fórmula empírica (notación de Hill):
C18H16FN3O
Número de CAS:
Peso molecular:
309.34
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77
203,00 €
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Productos recomendados
Nivel de calidad
Ensayo
≥98% (HPLC)
Formulario
liquid
fabricante / nombre comercial
Calbiochem®
condiciones de almacenamiento
OK to freeze
desiccated (hygroscopic)
protect from light
Condiciones de envío
wet ice
temp. de almacenamiento
2-8°C
cadena SMILES
Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1
InChI
1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
Clave InChI
VNDWQCSOSCCWIP-UHFFFAOYSA-N
Descripción general
A potent inhibitor of Janus Protein tyrosine Kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). It inhibits other kinases only at much higher concentrations. Also inhibits IL-2- and IL-4-dependent proliferation of CTLL cells and blocks the phosphorylation of STAT5.
Acciones bioquímicas o fisiológicas
Cell permeable: yes
Primary Target
murine JAK1
murine JAK1
Product competes with ATP.
Reversible: yes
Target IC50: 15 nM, 1 nM against murine JAK1 and JAK2, respectively; 1 nM against Tyk2
Target Ki: 5 nM against JAK3
Envase
Packaged under inert gas
Advertencia
Toxicity: Irritant (B)
Forma física
A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.
Reconstitución
Following initial use, aliquot and refrigerate (4°C).
Otras notas
Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.
Información legal
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de clase de almacenamiento
10 - Combustible liquids
Clase de riesgo para el agua (WGK)
WGK 2
Punto de inflamabilidad (°F)
188.6 °F - closed cup - (Dimethylsulfoxide)
Punto de inflamabilidad (°C)
87 °C - closed cup - (Dimethylsulfoxide)
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
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Nature cell biology, 19(10), 1164-1177 (2017-09-26)
Signalling downstream of Activin/Nodal (ActA) and Wnt can induce endoderm differentiation and also support self-renewal in pluripotent cells. Here we find that these apparently contradictory activities are fine-tuned by insulin. In the absence of insulin, the combination of these cytokines
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Can the InSolution JAK Inhibitor I - CAS 457081-03-7 - Calbiochem also target human JAK, considering that its primary target is stated as murine? I am in search of an inhibitor for human JAK.
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