A JAK2 inhibitor
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JAK Inhibitor 31

Item No. 39387

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[5-methyl-2-[(3-methyl-5-isothiazolyl)amino]-4-pyrimidinyl]-3-(4-methyl-1-piperazinyl)-3-azetidineacetonitrile
CAS Number
2891469-99-9
Synonyms
  • Janus-Associated Kinase Inhibitor 31
Molecular Formula
C19H26N8S
Formula Weight
398.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): Slightly soluble
λmax
226, 254, 286 nm
SMILES
CC1=C(N2CC(N3CCN(C)CC3)(CC#N)C2)N=C(NC4=CC(C)=NS4)N=C1
InChi Code
InChI=1S/C19H26N8S/c1-14-11-21-18(22-16-10-15(2)24-28-16)23-17(14)26-12-19(13-26,4-5-20)27-8-6-25(3)7-9-27/h10-11H,4,6-9,12-13H2,1-3H3,(H,21,22,23)
InChi Key
VGBYAYCYPVFDTM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    JAK inhibitor 31 is an inhibitor of JAK2 (IC50 = 3.9 nM).1 It is selective for JAK2 over JAK3 (IC50s = 70 nM), as well as Aurora B kinase, VEGFR2, Abl1, and GSK3β (IC50s = 0.441, 1.5, 21.37, and 50 µM, respectively), but does inhibit JAK1 and TYK2 (IC50s = 7 and 2.9 nM, respectively). JAK inhibitor 31 inhibits STAT3-mediated transcription of IL6 in a secreted alkaline phosphatase (SEAP) reporter assay (IC50 = 162 nM). It reduces ocular inflammation, as well as decreases Il6 expression in the meibomian glands, in a mouse model of allergic eye disease when used at concentrations of 1 or 3 mg/ml.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gordhan, H.M., Miller, S.T., Clancy, D.C., et al. Eyes on topical ocular disposition: The considered design of a lead Janus kinase (JAK) inhibitor that utilizes a unique azetidin-3-amino bridging scaffold to attenuate off-target kinase activity, while driving potency and aqueous solubility. J. Med. Chem. 66(13), 8929-8950 (2023).