Art. -Nr.: HY-18629

SU9516

Name: SU9516
Brand: MedChemExpress
SKU: HY-18629
Price: 40.00 USD
Availability: InStock
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5 Cited Publications

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Based on 5 publication(s) in Google Scholar

SU9516 is a potent CDK2 inhibitor, with an IC₅₀ of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC₅₀s of 40, 200 nM, respectively.

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Reinheit : 99.85%
CAS. Nr.: 377090-84-1
Formel: C₁₃H₁₁N₃O₂
Molecular Weight:241.25

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SU9516 Chemical Structure

CAS. Nr.: 377090-84-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SU9516 is a potent CDK2 inhibitor, with an IC₅₀ of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC₅₀s of 40, 200 nM, respectively.

IC₅₀ & Target

^[1]

CDK2

22 nM (IC₅₀)

CDK1

40 nM (IC₅₀)

CDK4

200 nM (IC₅₀)

PDGFr

18000 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.022 μM Compound: SU9516	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	0.026 μM Compound: SU9516	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	0.168 μM Compound: SU9516	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	0.905 μM Compound: SU9516	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	1.5 μM Compound: SU9516	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	1.6 μM Compound: SU-9516	Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells	[PMID: 20117004]
Sf9	IC₅₀	1.7 μM Compound: SU9516	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]

In Vitro

SU9516 shows slight activities against PKC, p38, PDGFr and EGFR, with IC₅₀ of >10, >10, 18, and >100 μM. SU9516 (5 μM) decreases cdk2-specific Phosphorylation of pRB and inhibits cell cycle progression in RKO cells. SU9516 (5 μM) also induces apoptosis in RKO and SW480 Cells^[1]. SU9516 (5 μM) results in enhanced pRb/E2F complex formation in HT-29 cells. SU9516 enhances presence of E2F species in multiprotein complexes^[2]. SU9516 (5 μM) rapidly induces cytochrome crelease, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1. SU9516 causes down-regulation of Mcl-1 mRNA levels in human leukemia cells. Furthermore, SU9516 treatment results in a marked increase in reactive oxygen species production^[3].

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

Chemical Information

CAS. Nr. 377090-84-1
Appearance Solid
Molecular Weight 241.25
Formel C₁₃H₁₁N₃O₂
Color Orange to reddish brown
SMILES

O=C1NC2=C(C=C(OC)C=C2)/C1=C/C3=CN=CN3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
J Exp Clin Cancer Res

Wilms' tumor 1-associating protein promotes renal cell carcinoma proliferation by regulating CDK2 mRNA stability. [Abstract]

2018 Feb 27;37(1):40. PMID: 29482572
Cell Death Differ

p53-dependent elimination of aneuploid mitotic offspring by entosis. [Abstract]

2021 Feb;28(2):799-813. PMID: 33110215
J Biosci Bioeng

Effect of cell-extracellular matrix interaction on myogenic characteristics and artificial skeletal muscle tissue. [Abstract]

2020 Jul;130(1):98-105. PMID: 32278672
bioRxiv

2020 Feb.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (414.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

4.1451 mL

20.7254 mL

41.4508 mL

5 mM

0.8290 mL

4.1451 mL

8.2902 mL

10 mM

0.4145 mL

2.0725 mL

4.1451 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, 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.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.25 mg/mL (13.47 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 3.25 mg/mL (13.47 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 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 (32.5 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

Protokoll

Kinase Assay^[1]

Kinase assays are performed in 96-well polypropylene plates. Each reaction contains 2 μg of histone H1 at a final concentration of 10 μM [-³³P]ATP (0.2 μCi/well), 10 mM MgCl₂,1mM DTT, 0.01% Triton X-100, and 10% glycerol in a 40 μL volume. The reaction is initiated with the addition of 20 μL enzyme (6 ng cdk2/well resulting in a final concentration of 1.6 nM), which is previously diluted 1:50-1:200 in the same buffer, and allowed to proceed for 1 h at room temperature. Reaction is stopped by the addition of 0.01 mL 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is washed three times with 1.0% phosphoric acid, air dried, and then counted for radioactivity in a liquid scintillation counter.

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

Cell Assay^[1]

RKO cells and SW480 cells are seeded in replicates (n = 6) in 96-well plates at 1×10⁴ cells/well and allowed to attach overnight. SU9516 is added in concentrations from 0.05 μM to 50.00 μM for 24 h, the cells are then washed twice with PBS, and cells are replenished with complete media. The cells are fixed at 0, 4, and 7 days post-drug removal and assayed for protein levels using a modified SRB cytotoxicity assay. The cells are fixed in 10% trichloroacetic acid for 1 h, washed in distilled H₂O, and stained in 0.4% SRB/acetic acid for 30 min. The cells are then washed in 0.1% acetic acid, solubilized in 10 mM Tris (pH 9), and analyzed on a Bio-Rad 360 microplate reader at 595 nm. All experiments are repeated at least three times.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Lane ME, et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7. [Content Brief]

[2]. Yu B, et al. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem Pharmacol. 2002 Oct 1;64(7):1091-100. [Content Brief]

[3]. Gao N, et al. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism. Mol Pharmacol. 2006 Aug;70(2):645-55. [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, 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	4.1451 mL	20.7254 mL	41.4508 mL	103.6269 mL
	5 mM	0.8290 mL	4.1451 mL	8.2902 mL	20.7254 mL
	10 mM	0.4145 mL	2.0725 mL	4.1451 mL	10.3627 mL
	15 mM	0.2763 mL	1.3817 mL	2.7634 mL	6.9085 mL
	20 mM	0.2073 mL	1.0363 mL	2.0725 mL	5.1813 mL
	25 mM	0.1658 mL	0.8290 mL	1.6580 mL	4.1451 mL
	30 mM	0.1382 mL	0.6908 mL	1.3817 mL	3.4542 mL
	40 mM	0.1036 mL	0.5181 mL	1.0363 mL	2.5907 mL
	50 mM	0.0829 mL	0.4145 mL	0.8290 mL	2.0725 mL
	60 mM	0.0691 mL	0.3454 mL	0.6908 mL	1.7271 mL
	80 mM	0.0518 mL	0.2591 mL	0.5181 mL	1.2953 mL
	100 mM	0.0415 mL	0.2073 mL	0.4145 mL	1.0363 mL

Bioz

Keywords

SU9516

5 Cited Publications

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SU9516

Publications Citing Use of MedChemExpress (MCE) SU9516

Alle CDK Isoform-spezifische Produkte anzeigen