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(s):
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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| Size/SKU | Availability | Price |
|---|---|---|
500 μg | Available to ship TODAYfromAreál Kühne+Nagel spol. s r.o. | CZK 3,920.00 |
About This Item
Empirical Formula (Hill Notation):
C18H16FN3O
CAS Number:
Molecular Weight:
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
CZK 3,920.00
Available to ship TODAYDetails
Product Name
JAK Inhibitor I, InSolution, ≥98%
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
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.
Biochem/physiol Actions
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
Packaging
Packaged under inert gas
Physical form
A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.
Preparation Note
Following initial use, aliquot and refrigerate (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
Toxicity: Irritant (B)
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This Item | |||
|---|---|---|---|
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥97% (HPLC) | assay ≥98% (HPLC) |
| form liquid | form solid | form solid | form solid |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
| manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® | manufacturer/tradename Calbiochem® |
| 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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Storage Class
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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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.
1 answer-
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