An inhibitor of MRCKα and MRCKβ
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BDP9066

Item No. 26264

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-8-[3-(4-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1,8-diazaspiro[5.5]undecane
CAS Number
2226507-04-4
Molecular Formula
C20H24N6
Formula Weight
348.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
C1(C(C2=NC=NC=C2)=CN3)=C3N=CC=C1N4C[C@@]5(NCCCC5)CCC4
InChi Code
InChI=1S/C20H24N6/c1-2-8-25-20(6-1)7-3-11-26(13-20)17-5-10-22-19-18(17)15(12-23-19)16-4-9-21-14-24-16/h4-5,9-10,12,14,25H,1-3,6-8,11,13H2,(H,22,23)/t20-/m0/s1
InChi Key
UELSMLDRSQFVHG-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $162

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    10 mg

    $270

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    Product Description

    BDP9066 is an inhibitor of Cdc42-binding kinase α (MRCKα) and MRCKβ (Kis = 0.0136 and 0.0233 nM, respectively).1 It is selective for MRCKα and MRCKβ over Rho-associated kinase 1 (ROCK1) and ROCK2 (Kis = 18.4 and 5.38 nM, respectively) and a panel of 115 additional kinases at 1 µM. BDP9066 has antiproliferative activity against a panel of 757 cancer cell lines (EC50s = <10 µM). It inhibits the phosphorylation of myosin light-chain 2 (MLC2) in SCC-12 squamous cell carcinoma cells (EC50 = 64 nM) and inhibits the motility of the same cells. BDP9066 (25 µg/animal) decreases average papilloma volume in a mouse two-stage model of skin carcinogenesis initiated by 7,12-dimethylbenz[a]anthracene (DMBA; Item No. 30383) and promoted by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Unbekandt, M., Belshaw, S., Bower, J., et al. Discovery of potent and selective MRCK inhibitors with therapeutic effect on skin cancer. Cancer Res. 78(8), 2096-2114 (2018).