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
≥98% (HPLC), liquid
Synonym(e):
InSolution JAK-Inhibitor I, 2-(1,1-Dimethylethyl)-9-fluor-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-on, P6, Pyridon 6, DBI, JAK1-Inhibitor I, JAK2-Inhibitor I, JAK3-Inhibitor X
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| Ihnen/SKU | Verfügbarkeit | Preis |
|---|---|---|
500 μg | Warenkorb auf Verfügbarkeit prüfen | € 153,00 |
Über diesen Artikel
Empirische Formel (Hill-System):
C18H16FN3O
CAS-Nummer:
Molekulargewicht:
309.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
liquid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
€ 153,00
Warenkorb auf Verfügbarkeit prüfen
Technischer Dienst
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Unterstützung erhaltenProduktname
JAK-Inhibitor I, InSolution
Quality Segment
assay
≥98% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
shipped in
wet ice
storage temp.
2-8°C
SMILES string
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)
InChI key
VNDWQCSOSCCWIP-UHFFFAOYSA-N
General description
Ein starker Inhibitor von Janus-Protein-Tyrosin-Kinasen (JAK). Zeigt eine starke Hemmaktivität gegenüber JAK1 (IC50 = 15 nM für JAK1 der Maus), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM) und Tyk2 (IC50 = 1 nM). Hemmt andere Kinasen nur in deutlich höheren Konzentrationen. Hemmt zudem die IL-2- und IL-4-induzierte Proliferation von CTLL-Zellen und blockiert die Phosphorylierung von STAT5.
Biochem/physiol Actions
Primärziel
JAK1 der Maus
JAK1 der Maus
Produkt konkurriert mit ATP.
Reversibel: ja
Zellpermeabel: ja
Ziel Ki: 5 nM gegen JAK3
Ziel-IC50: 15 nM, und 1 nM gegen JAK1 bzw. JAK2 der Maus; 1 nM gegen Tyk2
Packaging
Verpackt unter inertem Gas
Physical form
Eine 10 mM Lösung (500 µ;g/162 µ;l) von JAK-Inhibitor I (Best.-Nr. <;A href="https://./?[islink]ViewProductDetail-BySKU&;#124;&;#124;SKU&;#124;EMD_BIO-420099&;#124;[/islink]">;420099<;/A>;) in DMSO.
Preparation Note
Nach dem ersten Gebrauch in Aliquote aufteilen und kühlen (4 °;C).
Other Notes
Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxizität: Reizstoff (B)
1 of 1
Dieser Artikel | |||
|---|---|---|---|
| description InSolution | description JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC50 = 15 nM), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC50 = 1 nM). | description The JAK2 Inhibitor IV, also referenced under CAS 1110502-30-1, controls the biological activity of JAK2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. | description The JAK3 Inhibitor VI, also referenced under CAS 856436-16-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥97% (HPLC) | assay ≥98% (HPLC) |
| form liquid | form solid | form solid | form solid |
| manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
| storage temp. 2-8°C | storage temp. −20°C | storage temp. 2-8°C | storage temp. 2-8°C |
| storage condition OK to freeze, protect from light, desiccated (hygroscopic) | storage condition OK to freeze, protect from light | storage condition OK to freeze, protect from light | storage condition OK to freeze, desiccated (hygroscopic), protect from light |
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Lagerklasse
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
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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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