2. PROTAC Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Apoptosis Caspase Aurora Kinase
  4. SK2188

SK2188 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: AURKA ligand: MK-5108 (HY-13252); Blue: Thalidomide (HY-14658); Black: Linker: Amino-PEG4-alcohol (HY-W008005)).

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

SK2188 Chemical Structure

SK2188 Chemical Structure

CAS No. : 3038446-94-2

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SK2188 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Aurora Kinase Aurora A Aurora B Aurora C

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Description

SK2188 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: AURKA ligand: MK-5108 (HY-13252); Blue: Thalidomide (HY-14658); Black: Linker: Amino-PEG4-alcohol (HY-W008005))[1].

IC50 & Target[1]

Caspase 3

 

Caspase-7

 

Aurora A

 

Cereblon

 

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.

SK2188 Related Antibodies

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.
Molecular Weight

893.38

Formula

C43H46ClFN6O10S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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SK2188 Related Classifications

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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.

Keywords:

SK21883038446-94-2JB325SK 2188SK-2188JB 325JB-325PROTACsApoptosisCaspaseAurora KinaseNGP cellsAURKANeuroblastomaMYCNInhibitorinhibitorinhibit

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