A CK1α inhibitor
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Casein Kinase Inhibitor A51

Item No. 44831

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-N-[5-chloro-4-[5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl]-2-pyrimidinyl]-1,4-cyclohexanediamine
CAS Number
2079068-74-7
Synonyms
  • BTX-A51
Molecular Formula
C18H25ClN6
Formula Weight
360.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CN1N=CC(C2=NC(N[C@H]3CC[C@@H](CC3)N)=NC=C2Cl)=C1CC4CC4
InChi Code
InChI=1S/C18H25ClN6/c1-25-16(8-11-2-3-11)14(9-22-25)17-15(19)10-21-18(24-17)23-13-6-4-12(20)5-7-13/h9-13H,2-8,20H2,1H3,(H,21,23,24)/t12-,13-
InChi Key
RVZJFCNYSSUDCU-JOCQHMNTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Casein kinase inhibitor A51 is an inhibitor of casein kinase 1α (CK1α).1 It binds to CK1α, CK1δ, and CK1ε (Kds = 5.3, 1.8, and 4.4 nM, respectively) and reduces phosphorylation of β-catenin at serine 45, a site phosphorylated specifically by CK1α, when used at a concentration of 1 µM. Casein kinase inhibitor A51 (27 nM) inhibits the proliferation of bone marrow cells isolated from mice with acute myeloid leukemia (AML) driven by the oncogenic fusion protein MLL-AF9. It rapidly increases intratumoral levels of p53 and induces intratumoral apoptosis in a murine model of MLL-AF9-driven AML. Casein kinase inhibitor A51 (5 mg/kg per day) also increases survival and eradicates signs of disease in the same model over five months.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Minzel, W., Venkatachalam, A., Fink, A., et al. Small molecules co-targeting CKIα and the transcriptional kinases CDK7/9 control AML in preclinical models. Cell 175(1), 185.e125 (2018).