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K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $98 | 6-8 weeks | |
5 mg | $265 | 6-8 weeks | |
25 mg | $920 | 6-8 weeks | |
50 mg | $1,180 | 6-8 weeks | |
100 mg | $1,820 | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $320 | 6-8 weeks |
Description | K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases. |
Targets&IC50 | CLK1:8.9 nM, ERK2:1.0 μM, PDGFRβ:1.6 μM, CLK3:29.2 nM, CDK2-CyclinA:0.5 nM, Calmodulin kinase:8.9 μM, Casein kinase-1:2.8 μM, PKA:5.2 μM, CDK1-CyclinB:0.6 nM, GSK-3:0.14 μM, VEGFR2:0.032 μM |
In vitro | K 00546 binds to the SLK ATP binding site and forms three hydrogen bonds with the kinase hinge residues E109 and C111. In addition, the aminosulfonyl portion of K 00546 interacts with the backbone of L40. [1] K 00546 also inhibits a number of kinases, including PKA, casein kinase-1, MAP kinase (ERK-2), calmodulin kinase, VEGF-R2, GSK-3, and PDGF-Rβ, with IC50 values of 5.2 μM, 2.8 μM, 1.0 μM, 8.9 μM, 0.032 μM, 0.14 μM, and 1.6 μM, respectively. K 00546 is a potent CDK1 and CDK2 inhibitor with IC50 values of 0.6 nM for CDK1/cyclin B and 0.5 nM for CDK2/cyclin A. [2] K 00546 has also been shown to be a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50 values of 8.9 nM and 29.2 nM, respectively. [3] |
Alias | K00546 |
Molecular Weight | 425.44 |
Formula | C15H13F2N7O2S2 |
Cas No. | 443798-47-8 |
Smiles | O=S(=O)(N)C1=CC=C(C=C1)NC=2N=C(N)N(N2)C(=S)NC=3C(F)=CC=CC3F |
Relative Density. | 1.72 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (188.04 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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