A Clk1 and Clk2 inhibitor
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SGC-CLK-1

Item No. 41311

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(6-methoxypyrazolo[1,5-b]pyridazin-3-yl)-N-[3-methoxy-5-(trifluoromethyl)phenyl]-2-pyrimidinamine
CAS Number
748142-15-6
Synonyms
  • CAF-170
  • CDC-like Kinase 1
Molecular Formula
C19H15F3N6O2
Formula Weight
416.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC(F)(C1=CC(NC2=NC=CC(C3=C(C=CC(OC)=N4)N4N=C3)=N2)=CC(OC)=C1)F
InChi Code
InChI=1S/C19H15F3N6O2/c1-29-13-8-11(19(20,21)22)7-12(9-13)25-18-23-6-5-15(26-18)14-10-24-28-16(14)3-4-17(27-28)30-2/h3-10H,1-2H3,(H,23,25,26)
InChi Key
GJYVLTPTDBQQCY-UHFFFAOYSA-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

    SGC-CLK-1 is an inhibitor of CDC-like kinase 1 (Clk1) and Clk2 (IC50s = 13 and 4 nM, respectively).1 It is selective for Clk1 and Clk2 over Clk3, Clk4, homeodomain-interacting protein kinase 1 (HIPK1), HIPK2, and serine/threonine kinase 16 (STK16; IC50s = 363, 46, 50, 42, and 49 nM, respectively). SGC-CLK-1 (1 µM) inhibits the proliferation of MDA-MB-435 breast cancer and U-118 MG glioma cells. It induces diffuse localization of Clk2 and phosphorylated serine/arginine-rich (pSR) proteins, targets of Clks, without reducing the levels of phosphorylated SR proteins in MDA-MB-435 and U-118 MG cells when used at a concentration of 500 nM. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tiek, D., Wells, C.I., Schröder, M., et al. SGC-CLK-1: A chemical probe for the Cdc2-like kinases CLK1, CLK2, and CLK4. Curr. Res. Chem. Biol. 3, 100045 (2023).