CK1δ Inhibitor, SR-1277

A cell-permeable, brain permeant, purine derivative that acts as a potent, ATP-competitive inhibitor of CK1δ (IC₅₀ = 49 nM; K_i = 69 nM). Inhibits CK1δ, FLT3, Cdk6/Cyclin D3 and Cdk9/Cyclin K, but with reduced potency (IC₅₀ = 260, 305, 311, and 260 nM, respectively). Suppresses the proliferation of cerebellar granule cell progenitors (GCPs), without inducing cell death. Also reduces the expression on sonic hedgehog (Shh; 75 ng/ml)-induced Ccna1, Ccnb1, Ccnd2, Ccne1, Cdkn1a, and Cdkn1b mRNA in GCPs (~ 100 nM). Displays anti-proliferative effect in A375 melanoma cells (EC₅₀ = 22 nM in MTT assay) and in DAOY and D283 human medulloblastoma cell lines. Decreases proliferation of subcutaneously injected Ptch1+/- tumor cells allografts in mice (20 mg/kg, b,i.d).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
CK1δ

Reversible: yes

Target IC₅₀: 49 nM for CK&delta

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Bibian, M., et al. 2013. Bioorg. Med. Chem. Lett.23, 4374.

Penas, C., et al. 2015. Cell. Rep.11, 249.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)