JB170

JB170 : Degrader (PROTAC) of AURKA

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe JB170 is in the process of SERP review.

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Information

AURKA

Degrader (PROTAC)

300 nM

Probe Availability:

In Vitro Validations

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: Kd

Potency Value: 99 nM

Potency Assay: Kinobead assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

DOI Reference: 10.1038/s41589-020-00652-y

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: Kd

Potency Value: 183 ± 22 nM

Potency Assay: ITC of ternary complex

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

DOI Reference: 10.1038/s41589-020-00652-y

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): Kinobead selectivity profiling in MV4–11 cell lysates. JB170 bound AURORA-A with the lowest Kd (Kdapp = 99 nM), followed by ACAD10 (Kdapp = 253 nM) and AURORA-B (Kdapp = 5.1 µM).

Potency assay, off target (cells): MV4–11 cells were treated with JB170 (0.1 µM) for 6 h, and the proteins were analyzed by triple-SILAC MS. JB170 decreased AURORA-A levels by 73% compared to untreated cells: of the 4,259 proteins reliably detected in this experiment, no additional protein was depleted

Potency assay, off target (cells): In cell BRET assay shows that JB170 preferentially binds AURORA-A over AURORA-B (AURORA-A EC50 = 193 nM, AURORA-B EC50 = 1.4 µM).

Potency assay, off target (cells): Potency and specificity of JB170 was further evaluated via quantitative MS. On IMR5 cells, JB170 induces the specific, efficient degradation of AURORA-A compared to alisertib, and gave similar results when the effects of JB170 were compared to JB211, which resembles JB170 but cannot bind CEREBLON. JB170-mediated depletion is highly specific to AURORA-A.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Good specificity Aurora A degrader (only protein significantly degraded out of ~4K quantified by proteomics). Degradation is however incomplete and there are some emerging newer degraders available that likely show more potent DC50s for Aurora A.

(last updated: 6 Apr 2025 )