A RSK2 inhibitor with multiple off target effects
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

BIX 02565

Item No. 19183

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5R)-N-[1-[3-(dimethylamino)propyl]-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-5-methyl-1-oxo-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide
CAS Number
1311367-27-7
Molecular Formula
C26H30N6O2
Formula Weight
458.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
248, 335 nm
SMILES
O=C1C(N2[C@H](C)CCN1)=CC3=C2C=C(C(NC4=NC(C=CC=C5)=C5N4CCCN(C)C)=O)C=C3
InChi Code
InChI=1S/C26H30N6O2/c1-17-11-12-27-25(34)23-15-18-9-10-19(16-22(18)32(17)23)24(33)29-26-28-20-7-4-5-8-21(20)31(26)14-6-13-30(2)3/h4-5,7-10,15-17H,6,11-14H2,1-3H3,(H,27,34)(H,28,29,33)/t17-/m1/s1
InChi Key
ZHMXXVNQAFCXKK-QGZVFWFLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    500 µg

    $40

    Add

    1 mg

    $73

    Add

    5 mg

    $246

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    BIX 02565 is a RSK2 inhibitor with an IC50 value of 1.1 nM.1,2 It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors.1,2 BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).1 In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kirrane, T.M., Boyer, S.J., Burke, J., et al. Indole RSK inhibitors. Part 2: Optimization of cell potency and kinase selectivity. Bioorg. Med. Chem. Lett. 22(1), 738-742 (2012).

    2. Fryer, R.M., Muthukumarana, A., Chen, R.R., et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. J. Pharmacol. Exp. Ther. 340(3), 492-500 (2012).