A pan-JAK inhibitor
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JAK Inhibitor I

Item No. 15146

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(1,1-dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one
CAS Number
457081-03-7
Synonyms
  • CMP 6
  • Janus-Associated Kinase Inhibitor I
  • Pyridone 6
Molecular Formula
C18H16FN3O
Formula Weight
309.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 1 mg/ml
λmax
219, 260, 270, 328, 343, 359 nm
SMILES
O=C1NC=CC2=C1C(C=C(F)C=C3)=C3C4=C2NC(C(C)(C)C)=N4
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $104

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    10 mg

    $160

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    25 mg

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    Product Description

    Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.1,2 JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM - > 10 μM) for other protein tyrosine kinases.3 It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.3 In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Leonard, W.J., and O'Shea, J.J. Jaks and STATs: Biological implications. Annu. Rev. Immunol. 16, 293-322 (1998).

    2. Yamaoka, K., Saharinen, P., Pesu, M., et al. The Janus kinases (Jaks). Genome Biol. 5(12), 253 (2004).

    3. Thompson, J.E., Cubbon, R.M., Cummings, R.T., et al. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg. Med. Chem. Lett. 12(8), 1219-1223 (2002).

    4. Nakagawa, R., Yoshida, H., Asakawa, M., et al. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17. J. Immunol. 187(9), 4611-4620 (2011).

    Product Citations

    Wang, W., Green, M., Choi, J.E., et al. CD8+ T cells regulate tumour ferroptosis during cancer immunotherapy. Nature 569(7755), 270-274 (2019).