1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Stem Cell/Wnt PI3K/Akt/mTOR
  2. CDK VEGFR GSK-3
  3. K00546

K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively.

For research use only. We do not sell to patients.

K00546 Chemical Structure

K00546 Chemical Structure

CAS No. : 443798-47-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 339 In-stock
Solution
10 mM * 1 mL in DMSO USD 339 In-stock
Solid
5 mg USD 308 In-stock
10 mg USD 495 In-stock
50 mg USD 1430 In-stock
100 mg USD 2200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively[1][2][3].

IC50 & Target[1][2][3]

Cdk1/cyclin B

0.6 nM (IC50)

cdk2/cyclin A

0.5 nM (IC50)

CLK1

8.9 nM (IC50)

CLK3

29.2 nM (IC50)

VEGF-R2

32 nM (IC50)

GSK-3

140 nM (IC50)

In Vitro

K00546 binds to the SLK ATP-binding site forming three hydrogen bonds with the kinase hinge residues E109 and C111. The sulphamoyl moiety of K00546 also interacts with the main chain of L40[1].
K00546 (compound 3n) also inhibits 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

425.44

Formula

C15H13F2N7O2S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

S=C(N1N=C(NC2=CC=C(S(=O)(N)=O)C=C2)N=C1N)NC3=C(F)C=CC=C3F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (235.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3505 mL 11.7525 mL 23.5051 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3505 mL 11.7525 mL 23.5051 mL 58.7627 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 mL 11.7525 mL
10 mM 0.2351 mL 1.1753 mL 2.3505 mL 5.8763 mL
15 mM 0.1567 mL 0.7835 mL 1.5670 mL 3.9175 mL
20 mM 0.1175 mL 0.5876 mL 1.1753 mL 2.9381 mL
25 mM 0.0940 mL 0.4701 mL 0.9402 mL 2.3505 mL
30 mM 0.0784 mL 0.3918 mL 0.7835 mL 1.9588 mL
40 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4691 mL
50 mM 0.0470 mL 0.2351 mL 0.4701 mL 1.1753 mL
60 mM 0.0392 mL 0.1959 mL 0.3918 mL 0.9794 mL
80 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
100 mM 0.0235 mL 0.1175 mL 0.2351 mL 0.5876 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
K00546
Cat. No.:
HY-103647
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