K00546

Name: K00546
Brand: MedChemExpress
SKU: HY-103647
Rating: 4.5 (1 reviews)

Cat. No.: HY-103647 Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 443798-47-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 339	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 339	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 308	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1430	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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GSK-3 GSK-3α GSK-3β

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.0002 μM Compound: Fig.8B, R1C2	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.002 μM Compound: Fig.8B, R1C2	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.003 μM Compound: Fig.8B, R1C2	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.03 μM Compound: Fig.8B, R1C2	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.059 μM Compound: Fig.8B, R1C2	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.066 μM Compound: Fig.8B, R1C2	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]

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.

443798-47-8

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
10 mM	0.2351 mL	1.1753 mL	2.3505 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.08%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) HNMR (264 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Ashley C W Pike, et al. Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites. EMBO J. 2008 Feb 20;27(4):704-14. [Content Brief]

[2]. Ronghui Lin, et al. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11. [Content Brief]

[3]. Oleg Fedorov, et al. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol. 2011 Jan 28;18(1):67-76. [Content Brief]

Complete Stock Solution Preparation Table

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

K00546 Related Classifications

Help & FAQs

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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K00546

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K00546 Related Antibodies

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Complete Stock Solution Preparation Table

K00546 Related Classifications

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