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%
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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About This Item
Empirical Formula (Hill Notation):
C18H16FN3O
CAS Number:
Molecular Weight:
309.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Pricing and Inventory is not available. Please check the Merck website for more information.
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Quality Level
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
Warning
Toxicity: Irritant (B)
Physical form
A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.
Reconstitution
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
Storage Class Code
10 - Combustible liquids
WGK
WGK 2
Flash Point(F)
188.6 °F - closed cup - (Dimethylsulfoxide)
Flash Point(C)
87 °C - closed cup - (Dimethylsulfoxide)
Regulatory Listings
Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.
FSL
Group 4: Flammable liquids
Type 3 petroleums
Hazardous rank III
Water insoluble liquid
ISHL Indicated Name
Substances Subject to be Indicated Names
ISHL Notified Names
Substances Subject to be Notified Names
JAN Code
420097-500UG:
Certificates of Analysis (COA)
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Find documentation for the products that you have recently purchased in the Document Library.
Feras M Ghazawi et al.
Immunology and cell biology, 91(2), 149-158 (2012-12-05)
Interleukin (IL)-7 is an essential nonredundant cytokine, and throughout the lifespan of a T-cell signaling via the IL-7 receptor influences cell survival, proliferation and differentiation. It is therefore no surprise that expression of the IL-7 receptor alpha-chain (CD127) is tightly
Julia Ettich et al.
The Journal of biological chemistry, 299(11), 105270-105270 (2023-09-22)
Synthetic cytokine receptors can modulate cellular functions based on an artificial ligand to avoid off-target and/or unspecific effects. However, ligands that can modulate receptor activity so far have not been used clinically because of unknown toxicity and immunity against the
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes.
Arnold, et al.
International Journal of Molecular Sciences, 24 (2023)
Sandra March et al.
Nature protocols, 10(12), 2027-2053 (2015-11-20)
The development of therapies and vaccines for human hepatropic pathogens requires robust model systems that enable the study of host-pathogen interactions. However, in vitro liver models of infection typically use either hepatoma cell lines that exhibit aberrant physiology or primary
Kathryn G V Anderson et al.
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.
1 answer-
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