ML167

Catalog No.S7509

ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B.

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ML167 Chemical Structure

ML167 Chemical Structure
Molecular Weight: 335.36

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Quality Control & MSDS

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Product Description

Biological Activity

Description ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B.
Targets CLK4 [1] CLK1 [1] CLK2 [1] Dyrk1B [1]
IC50 136 nM 1522 nM 1648 nM 4420 nM
In vitro ML167, as a probe of Clk4, shows high cell permeability in a Caco-2 assay. [1]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Bioluminescent assay Two bioluminescent assays are used for the Clk4 assay. Measurement of ATP depletion is assessed by using the Kinase-Glo™ assay system, where a firefly luciferase detection reagent containing D-luciferin and buffer components are added to detect the remaining ATP, following the Clk4 kinase assay. The second system, ADP-Glo® measures kinase activity by quantifying the amount of ADP formed after the kinase reaction. Bioluminescent detection of ADP levels is achieved through the addition two different detection reagents. First, a reagent that stops the protein kinase reaction and depletes the remaining ATP is added. Then, a second reagent is added to stop ATP degradation. In addition, the second reagent also contains an enzyme, such as pyruvate kinase, that efficiently converts the ADP to ATP and the same firefly luciferase/D-luciferin components present in Kinase-Glo, which generate the luminescent signal proportional to the ADP concentration produced. Therefore, the two assay formats show opposite luminescent signal changes in response to protein kinase inhibitors.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rosenthal AS, et al. Probe Reports from the NIH Molecular Libraries Program. 2010.

Chemical Information

Download ML167 SDF
Molecular Weight (MW) 335.36
Formula

C19H17N3O3

CAS No. 1285702-20-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CID 44968231
Solubility (25°C) * In vitro DMSO 67 mg/mL (199.78 mM)
Ethanol 13 mg/mL warmed (38.76 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5-[4-[[(5-Methyl-2-furanyl)methyl]amino]-6-quinazolinyl]-2-furanmethanol

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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