An MSK1 inhibitor
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SB-747651A (hydrochloride)

Item No. 46111

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-4-piperidinyl-1H-imidazo[4,5-c]pyridine-7-methanamine, dihydrochloride
CAS Number
1781882-72-1
Molecular Formula
C16H22N8O • 2HCl
Formula Weight
415.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
NC1=NON=C1C2=NC3=CN=CC(CNC4CCNCC4)=C3N2CC.Cl.Cl
InChi Code
InChI=1S/C16H22N8O.2ClH/c1-2-24-14-10(8-20-11-3-5-18-6-4-11)7-19-9-12(14)21-16(24)13-15(17)23-25-22-13;;/h7,9,11,18,20H,2-6,8H2,1H3,(H2,17,23);2*1H
InChi Key
NRRCQHARLPNLHJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $46

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    5 mg

    $207

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    10 mg

    $322

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    25 mg

    $690

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    Product Description

    SB-747651A is an inhibitor of p90 ribosomal S6 kinase 1 (MSK1; IC50 = 0.5 nM).1 It is selective for MSK1 over Rho-associated kinase 1 (ROCK1), p70 ribosomal S6 kinase (p70S6K), dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), and cyclin-dependent kinase 2 (Cdk2; IC50s = 100, 270, 4,900, and >10,000 nM, respectively) and is greater than 300-fold selective over glycogen synthase kinase 3 (GSK3) and p90 ribosomal S6 kinase 1 (RSK1). SB-747651A (2 mg/kg, i.p.) reduces tumor volume and metastasis in a PANC-1 pancreatic cancer mouse xenograft model and reduces tumor volume in a patient-derived xenograft (PDX) mouse model of pancreatic cancer.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bamford, M.J., Bailey, N., Davies, S., et al. (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Further optimisation as highly potent and selective MSK-1-inhibitors. Bioorg. Med. Chem. Lett. 15(14), 3407-3411 (2005).

    2. Malvi, P., Chava, S., Cai, G., et al. HOXC6 drives a therapeutically targetable pancreatic cancer growth and metastasis pathway by regulating MSK1 and PPP2R2B. Cell Rep. Med. 4(11), 101285 (2023).