A kinase inhibitor
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MRT67307 (hydrochloride)

Item No. 19916

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]-cyclobutanecarboxamide, hydrochloride
Molecular Formula
C26H36N6O2 • XHCl
Formula Weight
464.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 3 mg/mlEthanol: 2 mg/ml
λmax
271 nm
SMILES
O=C(C1CCC1)NCCCNC2=NC(NC3=CC(CN4CCOCC4)=CC=C3)=NC=C2C5CC5.Cl
InChi Code
InChI=1S/C26H36N6O2.ClH/c33-25(21-5-2-6-21)28-11-3-10-27-24-23(20-8-9-20)17-29-26(31-24)30-22-7-1-4-19(16-22)18-32-12-14-34-15-13-32;/h1,4,7,16-17,20-21H,2-3,5-6,8-15,18H2,(H,28,33)(H2,27,29,30,31);1H
InChi Key
YBZGSNFTJJTIIO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $186

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    25 mg

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    Product Description

    MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s = 250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).1,2,3,4 MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages.1,3 Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Clark, K., Peggie, M., Plater, L., et al. Novel cross-talk within the IKK family controls innate immunity. Biochem. J. 434(1), 93-104 (2011).

    2. Clark, K., Takeuchi, O., Akira, S., et al. The TRAF-associated protein TANK facilitates cross-talk within the IkappaB kinase family during Toll-like receptor signaling. Proc. Natl. Acad. Sci. USA 108(41), 17093-17098 (2011).

    3. Clark, K., MacKenzie, K.F., Petkevicius, K., et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc. Natl. Acad. Sci. USA 109(42), 16986-16991 (2012).

    4. Petherick, K.J., Conway, O.J.L., Mpamhanga, C., et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. The Journal of Biological Chemisty 290(18), 11376-11383 (2015).