SK2188 free base · Synonyms: SK-2188 · SK 2188

SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC50 of 3.9 nM.

For research use only. Not for human or veterinary use.

Target PROTACs Aurora Kinase Apoptosis Caspase

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

SK2188 structure

CAS No.: 3038446-94-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 mg	USD 360.00	BP-02454-10mg	In stock	Get quote
25 mg	USD 720.00	BP-02454-25mg	In stock	Get quote
50 mg	USD 1,150.00	BP-02454-50mg	In stock	Get quote
100 mg	USD 1,840.00	BP-02454-100mg	In stock	Get quote
250 mg	USD 3,690.00	BP-02454-250mg	In stock	Get quote
500 mg	Inquire	BP-02454-500mg	In stock	Inquire

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Description

SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC50 of 3.9 nM. SK2188 recruits CRBN E3 ubiquitin ligase to target and degrade AURKA, abrogating both its catalytic and non-kinase functions, which leads to the destabilization and degradation of the oncogenic protein MYCN, ultimately inducing replication stress, DNA damage and apoptosis. SK2188 is applicable to research related to neuroblastoma .

Biological activity

In Vitro SK2188 (JB325) (0.1 nM-1 μM; 3-24 h) potently and selectively degrades AURKA in NGP neuroblastoma cells, with a DC50 of 3.9 nM. SK2188 (0.1 nM-1 μM; 24 h) induces apoptosis, specifically degrades AURKA, reduces MYCN, and upregulates pCHK1, pRPA32 and yH2AX to trigger replication stress and DNA damage in NGP cells. SK2188 (500 nM; 1-72 h) induces rapid and sustained degradation of AURKA protein in NGP cells, accompanied by time-dependent downregulation of MYCN protein. SK2188 (10 nM-10 μM; 48-120 h) potently inhibits the growth of MYCN-amplified NGP and IMR-32 neuroblastoma cells with IC50 values of 31.9 nM and 21.5 nM, respectively, but shows limited activity in N206 and SK-N-AS cells. It also potently reduces the cell viability of NB067 and NB139 neuroblastoma organoids with IC50 values of 26.4 nM and 131.3 nM, respectively, but exhibits limited activity in 000GKX and NB059 organoids.

Identifiers

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
InChIKey: YDRHAKKUUAJFHB-YCDNTZAYSA-N

Specifications

MW (average): 893.3760
Formula: C₄₃H₄₆ClFN₆O₁₀S
CAS No.: 3038446-94-2
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Rishfi M, et al. Targeted AURKA degradation: Towards new therapeutic agents for neuroblastoma. European journal of medicinal chemistry. 2023 Feb 05;247:115033.

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