Art. -Nr.: HY-107419

NU6140

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NU6140 is a selective CDK2-cyclin A inhibitor (IC₅₀, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs. NU6140 also potently inhibits Aurora A and Aurora B, with IC₅₀s of 67 and 35 nM, respectively. Enhances the apoptotic effect, with anti-cancer activity.

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Reinheit: 99.53%
CAS. Nr.: 444723-13-1
Formel: C₂₃H₃₀N₆O₂
Molecular Weight:422.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NU6140 Chemical Structure

CAS. Nr.: 444723-13-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

NU6140 is a selective CDK2-cyclin A inhibitor (IC₅₀, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs^[1]. NU6140 also potently inhibits Aurora A and Aurora B, with IC₅₀s of 67 and 35 nM, respectively^[2]. Enhances the apoptotic effect, with anti-cancer activity^[1]^[2].

IC₅₀ & Target^[1]^[2]

cdk2-cyclin A

0.41 μM (IC₅₀)

CDK1-Cyclin B

6.6 μM (IC₅₀)

CDK4-Cyclin D

5.5 μM (IC₅₀)

cdk5-p25

15 μM (IC₅₀)

cdk7-cyclin H

3.9 μM (IC₅₀)

Aurora A

67 nM (IC₅₀)

Aurora B

35 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.035 μM Compound: NU6140	Inhibition of GST-tagged AURORA B (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate Inhibition of GST-tagged AURORA B (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate	[PMID: 30234987]
Sf9	IC₅₀	0.067 μM Compound: NU6140	Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate	[PMID: 30234987]
Sf9	IC₅₀	0.94 μM Compound: NU6140	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	1.1 μM Compound: NU6140	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	2.3 μM Compound: NU6140	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]
Sf9	IC₅₀	5.1 μM Compound: NU6140	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	5.8 μM Compound: NU6140	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	8.8 μM Compound: NU6140	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]

In Vitro

NU6140 is less active on CDK1-cyclin B, CDK4-cyclin D, CDK5-p25 and CDK7-cyclin H, with IC₅₀s of 6.6, 5.5, 15 and 3.9 μM, respectively^[1].
NU6140 increases catalytic activity of capase-9 and capase-3, causes increase in the sub-G1 apoptotic cell population^[1].

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

Chemical Information

CAS. Nr. 444723-13-1
Appearance Solid
Molecular Weight 422.52
Formel C₂₃H₃₀N₆O₂
Color White to light yellow
SMILES

CCN(CC)C(C(C=C1)=CC=C1NC2=NC(OCC3CCCCC3)=C4C(N=CN4)=N2)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

bioRxiv

2019 Jan.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (591.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3668 mL

11.8338 mL

23.6675 mL

5 mM

0.4734 mL

2.3668 mL

4.7335 mL

10 mM

0.2367 mL

1.1834 mL

2.3668 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pennati M, et al. Potentiation of apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37. [Content Brief]

[2]. Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? Med Chem. 2018 Oct 25;61(20):9105-9120. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3668 mL	11.8338 mL	23.6675 mL	59.1688 mL
	5 mM	0.4734 mL	2.3668 mL	4.7335 mL	11.8338 mL
	10 mM	0.2367 mL	1.1834 mL	2.3668 mL	5.9169 mL
	15 mM	0.1578 mL	0.7889 mL	1.5778 mL	3.9446 mL
	20 mM	0.1183 mL	0.5917 mL	1.1834 mL	2.9584 mL
	25 mM	0.0947 mL	0.4734 mL	0.9467 mL	2.3668 mL
	30 mM	0.0789 mL	0.3945 mL	0.7889 mL	1.9723 mL
	40 mM	0.0592 mL	0.2958 mL	0.5917 mL	1.4792 mL
	50 mM	0.0473 mL	0.2367 mL	0.4734 mL	1.1834 mL
	60 mM	0.0394 mL	0.1972 mL	0.3945 mL	0.9861 mL
	80 mM	0.0296 mL	0.1479 mL	0.2958 mL	0.7396 mL
	100 mM	0.0237 mL	0.1183 mL	0.2367 mL	0.5917 mL

Keywords

NU6140

1 Cited Publications

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NU6140

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) NU6140

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NU6140

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) NU6140

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NU6140 Related Classifications

HY-107419 Related Classifications