Art. -Nr.: HY-171767

SK2188

(Synonyms: JB325)

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Based on 1 Customer Validation

SK2188 (JB325) is a highly efficient and selective PROTAC degrader targeting AURKA (DC₅₀ = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma.
(Pink: Aurora Kinase ligand (HY-13252); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.87%
CAS. Nr.: 3038446-94-2
Formel: C₄₃H₄₆ClFN₆O₁₀S
Molecular Weight:893.38

Speicherung:

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

SK2188 Chemical Structure

CAS. Nr.: 3038446-94-2

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Preis

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

SK2188 (JB325) is a highly efficient and selective PROTAC degrader targeting AURKA (DC₅₀ = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma^[1]. (Pink: Aurora Kinase ligand (HY-13252); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).

IC₅₀ & Target^[1]

Caspase 3

Caspase-7

Aurora A

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
IMR-32	IC₅₀	21.5 nM Compound: SK2188	Antiproliferative activity against human IMR-32 cells assessed as reduction in cell viability incubated for 48 hrs Antiproliferative activity against human IMR-32 cells assessed as reduction in cell viability incubated for 48 hrs	[PMID: 36549117]
SK-N-AS	IC₅₀	6693 nM Compound: SK2188	Antiproliferative activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs Antiproliferative activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs	[PMID: 36549117]

In Vitro

SK2188 (10-10000 nM, 48-120 h) efficiently inhibits proliferation in MYCN amplified cells and is effective in NB patient-derived organoids cells^[1].
SK2188 (10-1000 nM, 24 h) inhibits cell growth by inducing apoptosis in NGP cells^[1].
SK2188 (10-1000 nM, 24 h) degrades AURKA in NGP cells, triggering DNA damage and replication stress^[1].
SK2188 (100-1000 nM, 3h) has high target selectivity and degradation specificity in NGP cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

NGP cells, IMR-32 cells, N206 cells, SK-N-AS cells, NB patient-derived organoids cells
Concentration:

10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time:

48 h (NGP cells, IMR-32 cells, N206 cells, SK-N-AS cells); 120 h (NB patient-derived organoids cells)
Result:

Inhibited cell viability with IC₅₀s of 31.9 nM and 21.5 nM in NGP and IMR-32 cells, respectively, which were significantly lower than those of the parent inhibitor MK-5108 (IC₅₀s: 348.9 nM and 199.3 nM).
Inhibited cell viability with IC₅₀s of 131.3 nM and 26.4 nM in MYCN-amplified organoids NB139 and NB067, respectively, which were significantly lower than those of the parent inhibitor MK-5108 (IC₅₀s: 899.7 nM and 75.3 nM).

Apoptosis Analysis^[1]

Cell Line:

NGP cells
Concentration:

10 nM, 100 nM, 1000 nM
Incubation Time:

24 h
Result:

Significantly activated Caspase 3/7 at 10 nM and exerted a stronger apoptosis-inducing effect than MK-5108 at 1000 nM.

Western Blot Analysis^[1]

Cell Line:

NGP neuroblastoma cells
Concentration:

10 nM, 100 nM, 500 nM, 1000 nM
Incubation Time:

1 h, 3 h, 6 h, 24 h, 48 h, 72 h
Result:

Induced 89 % AURKA degradation (DC₅₀ = 3.9 nM) at 24 hours. Reduced MYCN protein levels (73 % degradation at 72 hours). Increased DNA damage markers (γH2AX, pCHK1)at 24 hours.

Chemical Information

CAS. Nr. 3038446-94-2
Appearance Solid
Molecular Weight 893.38
Formel C₄₃H₄₆ClFN₆O₁₀S
Color White to off-white
SMILES

O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(OCCOCCOCCOCCNC([C@@]4(CC[C@H](CC4)OC5=C(C(Cl)=CC=C5)F)CC6=CC=CC(NC7=NC=CS7)=N6)=O)=C3C1=O
Synonyms

JB325
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (111.93 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

1.1193 mL

5.5967 mL

11.1934 mL

5 mM

0.2239 mL

1.1193 mL

2.2387 mL

10 mM

0.1119 mL

0.5597 mL

1.1193 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (2.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (273 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Muhammad Rishf, et al. Targeted AURKA degradation: Towards new therapeutic agents for neuroblastoma. Eur J Med Chem. 2023 Feb 5:247:115033. [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	1.1193 mL	5.5967 mL	11.1934 mL	27.9836 mL
	5 mM	0.2239 mL	1.1193 mL	2.2387 mL	5.5967 mL
	10 mM	0.1119 mL	0.5597 mL	1.1193 mL	2.7984 mL
	15 mM	0.0746 mL	0.3731 mL	0.7462 mL	1.8656 mL
	20 mM	0.0560 mL	0.2798 mL	0.5597 mL	1.3992 mL
	25 mM	0.0448 mL	0.2239 mL	0.4477 mL	1.1193 mL
	30 mM	0.0373 mL	0.1866 mL	0.3731 mL	0.9328 mL
	40 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6996 mL
	50 mM	0.0224 mL	0.1119 mL	0.2239 mL	0.5597 mL
	60 mM	0.0187 mL	0.0933 mL	0.1866 mL	0.4664 mL
	80 mM	0.0140 mL	0.0700 mL	0.1399 mL	0.3498 mL
	100 mM	0.0112 mL	0.0560 mL	0.1119 mL	0.2798 mL

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SK2188

PROTAC Library

MCE Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SK2188

PROTAC Library

MCE Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SK2188 Related Classifications

HY-171767 Related Classifications