2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Aurora Kinase
  4. SK5527

SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research.
(Pink: Aurora A ligand (HY-179643); Blue: Cereblon E3 ligase ligand; Black: linker).

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

SK5527

SK5527 Chemical Structure

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SK5527 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Aurora Kinase Aurora A Aurora B Aurora C

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Description

SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research[1]. (Pink: Aurora A ligand (HY-179643); Blue: Cereblon E3 ligase ligand; Black: linker).

IC50 & Target[1]

Aurora A

2 nM (DC50)

In Vitro

SK5527 (0.01-10000 nM, 1-48 h) induces degradation AURKA MYCN in neuroblastoma and benign cell lines HEK293T, RPE), exhibits the high potency in MYCN-amplified cells (IMR-32, NGP, SJNB-8; SK-N-BE(2)-C with DC50s = 6 ,2 ,10 and 73 nM), shows reduced activity in other lines (SK-N-BE(2)-C, SK-N-AS, SJNB-1) with a hook effect, induces MYCN depletion as a secondary delayed consequence of AURKA degradation and requires concomitant engagement of both AURKA and CRBN to exert the degradation effect in MYCN amplified cells IMR-32, NGP, SJNB-8, SK-N-BE(2)-C with GI50s = 15, 21, 63, 477 nM;in non- amplified cells SK-N-SH, SK-N-AS and SJNB-1 with GI50s = 244, 654, 8635 nM; in benign immortalized cell RPE and HEK293T with GI50s = 460 and 408 nM[1].
SK5527 (10-10000 nM, 72 h) effectively inhibits neuroblastoma cells (IMR-32, NGP, SJNB 8 , SKN-SH, SK-N-BE(2)-C and SJNB-1) growth[1].
SK5527 (100-1000 nM, 3 h) requires both AURKA and CRBN binding for the activity, significantly engages AURKA with excellent kinome-wide selectivity, upregulates PLK1 and downregulates HAND2 and ESCO2 but GSPT1, CSNK1A1, ZFP91, SALL4, ZNF654, ZNF787, E4F1, and PATZ1[1].
SK5527 exhibites only modest inhibitory effects in the benign immortalized cell lines HEK293T and RPE, despite potent AURKA degradation, with GI50 values of approximately 0.5 μM[1].
SK5527 (10-1000 nM, 24-72 h) is limited by MDR1-Mediated Drug Efflux in SKN-SH, SK-N-BE(2)-C, SJNB-1, NGP, SJNB-8, IMR-32B but SK-N-AS (due to the low CRBN expression)[1].

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

SK5527 Related Antibodies

Western Blot Analysis[1]

Cell Line: IMR-32
Concentration: 500 nM
Incubation Time: 1, 4, 24 and 48 h
Result: Induced robust AURKA depletion already after 1 h, whereas MYCN co-depletion reached 50% only at 24h postexposure.

Cell Proliferation Assay[1]

Cell Line: IMR-32, NGP, SJNB 8 , SKN-SH, SK-N-BE(2)-C and SJNB-1
Concentration: 10, 100, 1000 and 10000 nM
Incubation Time: 72 h
Result: Had The strongest antiproliferative effects with GI50 values below 100 nM consistent with the observed potent AURKA degradation but less in SKN-SH, SK-N-BE(2)-C and SJNB-1.

Western Blot Analysis[1]

Cell Line: SK-N-BE(2)-C, SK-N-BE(2)-C, SK-N-SH, and SJNB-1
Concentration: 100 nM
Incubation Time: 24 h
Result: Exhibited high expression of multidrug resistance protein 1 (MDR1), encoded by the ABCB1 gene in SK-N-BE(2)-C, SK-N-SH, and SJNB-1.
Exhibited the highest MDR1 expression in our panel, cotreatment with 1 μM Tariquidar (HY-10550) significantly enhanced the AURKA degradation.

Cell Proliferation Assay[1]

Cell Line: NGP and SK-N-BE(2)-C cells
Concentration: 10, 100 and 1000 nM
Incubation Time: 48 h
Result: Dose-dependently increased of caspase 3/7 activity.

Cell Proliferation Assay[1]

Cell Line: NGP, SJNB-8, and SK-N-BE(2)-C
Concentration: 10, 100 and 1000 nM
Incubation Time: 72 h
Result: Exhibited growth-inhibitory activity comparable to AURKA inhibitor TAS-119, with nearly identical GI 50 values across cell lines.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax F C0 Vss
Mice[1] 15 mg/kg i.p. 2.7 h 1.0 h 6106 ng/mL 92 % / /
Mice[1] 15 mg/kg i.v. 2.2 h / / / 29221 ng/mL 1.1 L/kg
Mice[1] 2.5 mg/kg p.o. 2.5 h 0.5 h 2543 ng/mL 11 % / /
In Vivo

SK5527 (15 mg/kg, i.v. or i.p., once) induce AURKA protein depletion in IMR-32 neuroblastoma cell line-derived xenograft (CDX) mice[1].

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

Animal Model: IMR-32 cells (1 × 10 7 cells in 0.2 mL volume) induced-female BALB/c nude mice[1]
Dosage: 15 mg/kg
Administration: i.v., or i.p. once
Result: Reduced AURKA protein levels in vivo at 4 and 8 h post-treatment after a single IV dose, followed by a return to baseline levels at 24 h but not observed in i.p. group
Molecular Weight

848.36

Formula

C42H49ClF3N11O3
SMILES

FC1=CC=C(N=C1CC2(CCN(CC2)CC3=C(C(Cl)=CC=C3)F)C(N4CCC(F)(CN5CCN(C6=CC=C(C=N6)N7C(NC(CC7)=O)=O)CC5)CC4)=O)NC8=NNC(C)=C8
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SK5527 Related Classifications

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Help & FAQs
  • 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:

SK5527SK 5527SK-5527PROTACsAurora KinaseAURKA PROTAC degraderNanoLuc-AURKAMYCNneuroblasto2maInhibitorinhibitorinhibit

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