1. PROTAC
    Epigenetics
    Cell Cycle/DNA Damage
  2. PROTAC
    Aurora Kinase
  3. JB170

JB170 

Cat. No.: HY-141512
Handling Instructions

JB170 is a potent and highly specific PROTAC-mediated AURORA-A degrader (DC50=28 nM) by linking Alisertib, to the CEREBLON-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.

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

JB170 Chemical Structure

JB170 Chemical Structure

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Description

JB170 is a potent and highly specific PROTAC-mediated AURORA-A degrader (DC50=28 nM) by linking Alisertib, to the CEREBLON-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase[1].

IC50 & Target[1]

Aurora A

28 nM (DC50)

Aurora A

99 nM (Kd)

Aurora A

193 nM (EC50)

Cereblon

 

In Vitro

JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival[1].
JB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels [1].
JB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression[1].
JB170 (0.5 μM; 0-72 hours; MV4-11 cells) induced apoptosis is exclusively caused by targeting AURORA-A[1].
JB170 (0.1 µM; 0-9 hours; IMR5 cells) shows rapid AURORA-A depletion. JB170 (0~1 μM; 6 hours; MV4-11 cells) strongly attenuates in mutants with respect to AURORA-A. JB170 (0.1 μM; 18 hours; MV4-11 cells) does not activate AURORA-A. JB170 (0~1 µM; 24 hours; IMR5 cells) largely abrogates AURORA-AT217D depletion. JB170 (1 μM; 4 days; IMR5 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (IMR5 cells) reduces AURORA-A levels by lowering AURORA-A mRNA levels[1].

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

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 1 µM
Incubation Time: 24-72 hours
Result: After 72 hours, the number of viable cells was 32% of control levels.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.01~10 μM
Incubation Time: 6 hours
Result: Substantial degradation was observed at 100 nM and 1 µM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 µM
Incubation Time: 0~72 hours
Result: Apoptosis was exclusively caused by targeting AURORA-A.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 µM
Incubation Time: 12 hours
Result: Delayed or arrested S-phase progression.
Molecular Weight

963.36

Formula

C₄₈H₄₄ClFN₈O₁₁

SMILES

FC1=CC=CC(OC)=C1C2=NCC3=C(C4=C2C=C(C=C4)Cl)N=C(NC5=CC=C(C(OC)=C5)C(NCCOCCOCCNC(COC6=C7C(C(N(C7=O)C8CCC(NC8=O)=O)=O)=CC=C6)=O)=O)N=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

JB170JB 170JB-170PROTACAurora KinaseProteolysis-targeting chimeraAlisertibNon-catalyticMV4-11IMR5CancerAntitumorInhibitorinhibitorinhibit

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