A SIK inhibitor
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MR22

Item No. 9004611

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-(4-aminobutyl)-6-(2,5-difluorophenyl)-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
3027761-24-3
Molecular Formula
C18H19F2N5O
Formula Weight
359.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC1=CC=C(C=C1C2=CC3=C(N=C(N=C3)NC)N(C2=O)CCCCN)F
InChi Code
InChI=1S/C18H19F2N5O/c1-22-18-23-10-11-8-14(13-9-12(19)4-5-15(13)20)17(26)25(16(11)24-18)7-3-2-6-21/h4-5,8-10H,2-3,6-7,21H2,1H3,(H,22,23,24)
InChi Key
VCZDFACOFNRTMG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $32

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    5 mg

    $128

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    10 mg

    $208

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    25 mg

    $439

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    Product Description

    MR22 is an inhibitor of salt-inducible kinase (SIK; IC50s = 72, 89, and 18 nM for SIK1, SIK2, and SIK3, respectively).1 It is selective for SIK1-SIK3 over EPHA1-EPHA4 (IC50s = 0.145-2.1 µM), EPHB1-EPHB4 (IC50s = 0.607-22.6 µM), Abl1 (IC50 = 28.1 µM), JNK1 (IC50 = 23.2 µM), GAK (IC50 = 33.8 µM), and RSK1B (IC50 = >45 µM). MR22 (5 µM) induces cell cycle arrest at the G1 phase and reduces rapamycin-induced Akt phosphorylation in SKOV3 ovarian cancer cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rak, M., Tesch, R., Berger, L.M., et al. Shifting the selectivity of pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily. Eur. J. Med. Chem. 254, 115347 (2023).