An inhibitor of Cdk8 and Cdk19
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Senexin B

Item No. 28459

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[2-[6-[(4-methyl-1-piperazinyl)carbonyl]-2-naphthalenyl]ethyl]amino]-6-quinazolinecarbonitrile
CAS Number
1449228-40-3
Synonyms
  • SNX2-1-165
Molecular Formula
C27H26N6O
Formula Weight
450.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
218, 229, 327 nm
SMILES
O=C(N1CCN(C)CC1)C2=CC(C=CC(CCNC3=C(C=C(C#N)C=C4)C4=NC=N3)=C5)=C5C=C2
InChi Code
InChI=1S/C27H26N6O/c1-32-10-12-33(13-11-32)27(34)23-6-5-21-14-19(2-4-22(21)16-23)8-9-29-26-24-15-20(17-28)3-7-25(24)30-18-31-26/h2-7,14-16,18H,8-13H2,1H3,(H,29,30,31)
InChi Key
VNADJTWHOAMTLY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Senexin B is an inhibitor of Cdk8 and Cdk19.1 It inhibits Cdk8 with IC50 values ranging from 24 to 50 nM, depending on the assay used. It selectively inhibits Cdk19 and Cdk8 by 98.6 and 97.8%, respectively, in a panel of greater than 450 kinases at 2 μM but does inhibit MAP4K2 and YSK4 by 69 and 59%, respectively. Senexin B (1.25-5 μM) inhibits cell growth in MCF-7, BT474, and T47D-ER/Luc breast cancer cells in estrogen-containing media in a concentration-dependent manner.2 It reduces tumor growth in an MCF-7 mouse xenograft model when administered at a dose of 100 mg/kg twice per day. Senexin B (1 and 1.5 μM) also inhibits RANKL-induced differentiation of murine bone marrow-derived macrophages (BMDMs) into osteoclasts.3 It increases the bone volume fraction and bone mineral density in injured tibiae in a rat model of cancellous bone injury and regeneration when administered locally at a dose of 1 μg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Roninson, I.B., Porter, D.C., and Wentland, M.P. Cdk8-cdk19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer. (2016).

    2. McDermott, M.S., Chumanevich, A.A., Lim, C.-U., et al. Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer. Oncotarget 8(8), 12558-12575 (2017).

    3. Amirhosseini, M., Bernhardsson, M., Lång, P., et al. Cyclin-dependent kinase 8/19 inhibition suppresses osteoclastogenesis by downregulating RANK and promotes osteoblast mineralization and cancellous bone healing. J. Cell. Physiol. 234(9), 16503-16516 (2019).