An inhibitor of RSK1-4
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BI-D1870

Item No. 15264

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridinone
CAS Number
501437-28-1
Molecular Formula
C19H23F2N5O2
Formula Weight
391.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
262, 296 nm
SMILES
OC1=C(F)C=C(NC2=NC(N(CCC(C)C)C(C)C(N3C)=O)=C3C=N2)C=C1F
InChi Code
InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
InChi Key
DTEKTGDVSARYDS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $62

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    5 mg

    $222

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    10 mg

    $355

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    Product Description

    The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility.1 BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively).2 At 100 nM, it also significantly inhibits polo-like kinase 1, Aurora B, maternal embryonic leucine zipper kinase, and mammalian STE20-like kinase 2.2,3 BI-D1870 acts at the N-terminal kinase domain, but not the C-terminal domain, of RSK.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Romeo, Y., Zhang, X., and Roux, P.P. Regulation and function of the RSK family of protein kinases. Biochem. J. 441(2), 553-569 (2012).

    2. Sapkota, G.P., Cummings, L., Newell, F.S., et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J. 401(1), 29-38 (2007).

    3. Bain, J., Plater, L., Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochem. J. 408(3), 297-315 (2007).